Sulfur compounds pesticidal compositions containing them and method of their application

Ref: 4060/96 118481/2 IWO’yA’ no’vn jniN o’b’onn tnpm ’Ρυιρ triton ,rp-i£» nuionn

SULFUR COMPOUNDS, PESTICIDAL COMPOSITIONS CONTAINING THEM AND METHOD OF THEIR APPLICATION 118481/2 ί

The present invention relates to new sulfur compounds, including sulfilimines and 5 sulfoximines. The invention further pertains to compositions of said compounds and methods, using said compounds, for the control of arthropod, nematode, helminth or protozoan pests. Furthermore, it pertains to the application of compounds or compositions thereof in agricultural methods of use, particularly as pesticides.

In the instant specification, the word sulfilimine is used to name compounds 10 comprising the group the instant specification, the word sulfoximine is used to \(Ο)=34— name compounds comprising ' .

Various pesticidal pyrazoles, pyrroles, and imidazoles have been disclosed: European Patent Publication No 418016; European Patent Publication No 403309; U.S. Patent 5,104,994; European Patent Publication No 352944; U.S. Patent 5,079,370; U.S. Patent 15 5,047,550; U.S. Patent 5,232,940; U.S. Patent 4,810,720; U.S. Patent 4,804,675; U.S. Patent 5,306,694; U.S. Patent 4,614,533; WPO Publication No. WO 93/06089; and WPG Publication No. WO 94/21606 describe pesticidal (4-pyrazolyl) sulfides, sulfoxides and sulfones. U.S. Patent 5,187,185 describes 4-pyrrolyl sulfides, sulfoxides and sulfones. U.S. Patent 5,223,525 describes pesticidal 4-imidazolyl sulfides, sulfoxides and sulfones. 2 0 Due to the many existing pests and crops and conditions of attacks of crops by pests, there is a need for further novel pesticidal compounds. lh one aspect, the present invention provides compounds for use in controlling arthropod, nematode, helminth and protozoan pests, said compounds having the general formula: 25' XZR2 n1/\o

Fl· Q (I) or NH. 1 m© z m

OD 30 2 wherein: 5 =X is =NR3, =0 or an electron pair (it being understood that, in this situation, another way to represent Formula (I) is to delete =X); R1 is CrC6 alkyl, C3-Cg cycloalkyl, or C4-C8 (cycloalkyl)alkyl, each of which is optionally substituted by one or more halogen; R2 and R3 are independently selected from H; CrC6 alkyl; C/-C6 haloalkyl; COR4; 10 S(O)PR4; CN; N02; COOR4; CONR4R5; C(O)SR4; C(S)OR4; SO2NR4R5; P(O)q(R4)(R5); P(O)q(OR4)(R5); P(O)q(OR4)(OR5); C=(NR4)NR5R6; CH=NR4; C=(NR4)(OR5); C(S)N(R4)(R5); C(O)C(O)R4; C(0)C(0)0R4; C(O)C(O)NR4R5; and CONR4SO2R5; m is 1 or 2; p is 0, 1 or 2; 15 qisOorl; R4, R5 and R6 are independently selected from H; NO2; CN; CHO; R14; phenyl optionally substituted by one or more of R14, halogen, CN, N02, OR14, SR14, COR14, COOR14, or OR14; halogen; COR14; COOR14; CHO; and OH; Q is Q-l, Q-2 or Q-3, as designated below:

<img img-format="tif" img-content="drawing" file="IL118481AD00021.tif" id="idf0001" />

R7 is CN, NO2, H, CrC4 alkyl, CrC4 haloalkyl, halogen, CHO, or COR20, R7; 20 3 R8 is H, halogen, CN, S(O)pR14, OR4, NR16R17, N(RI6)CON(RI7)(R18), N3 or NH(Cr C5 alkyl) substituted by one or more OH, OR14, S(O)pR14, CN, NO2, COOR14 or CON(RI6)(R17); R9 and R*1 are independently selected from H, halogen, OR14, SR14 and R14; R10 is CN; R12 is H, halogen, R14, OR14, S(O)pR14 or R13 is H, halogen or

Ar is phenyl, optionally bearing one or more substituents selected from the group consisting of halogen, R15, OR15, SF5 and S(O)pR15; or Ar is 2-pyridyl, optionally bearing one or more substituents selected from the group consisting of halogen, R15, OR15, SF5 and S(O)PR14; R14 and R19 are independently selected from Q-Cg alkyl, C3-C6 cycloalkyl, and C4-C8 (cycloalkyl)alkyl, each of which is optionally substituted by one or more halogen; R15 is CrC6 alkyl, optionally substituted by one or more halogen; R16, R17 and R18 are independently selected from H, NO2, CN, CHO, R19, COR19, and COOR19; R20 is selected from CrC6 alkyl, optionally substituted by one or more halogen; and Z is an anionic counter ion, such as Cl", Br", Γ, F", OSO2R4", C1O4", OCOR4", BF4", SbF6", SO3” or HSO4‘, a phosphate anion or a hydrogenophosphate anion or other agriculturally acceptable anion.

The stereoisomers, e.g. diastereomers and optical isomers, having the Formula (I) or (Π) are included in the invention as well.

Preferred compounds of the present invention include one or more of the following features: (1) R1 is optionally halogenated CrC6 alkyl, preferably methyl or ethyl; and/or 4 (2) R2 is H, COOR4, S(O)pR4, CONR4R5, CN, COR4, P(O)q(OR4)(OR5) or P(O)q(R4)(R5); more preferably R2 is H; or CN; or COOR4 (in which R4 is CrC6 alkyl); or R' is S(O)pR4 (in which p is two and R4 is Ci-Cg alkyl or optionally substituted phenyl); or R2 is CONR4R5 (in which R4 is H or Ci-C6 alkyl and R5 is C(-C6 alkyl, or in which R4 is H and R5 is COR14 in which R14 is optionally halogenated CrC6 alkyl); or R2 is COR4 (in which R4 is H or C,-C6 alkyl); or R2 is P(O)q(OR4)(OR5) or P(O)q(R4)(R5) (in which q is one and R4 and R5 are each CrC6 alkyl) ;and/or (3) Q is Q-l,preferably wherein R7 is CN or H, or CrC4 alkyl and/or when R8 is N(RI6)(R17), most preferably when R8 is NH2;and/or (4) Ar is phenyl substituted in the 2 and 6 positions by halogen and in the 4 position by halogenated C)-C6 alkyl or SF5 or OR15, preferably when Ar is 2,6-dichloro-4-trifluoromethylphenyl; or Ar is 2-pyridyl substituted in the 3 position by halogen and in the 5 position by halogenated CrC6 alkyl or SF5 or OR15, preferably when Ar is 3-chloro-5-trifluoromethylpyrid-2-yl.

In another aspect, the present invention provides a pesticidal composition (i.e. an arthropodicidal, nematocidal, anti-helminth or anti-protozoal composition) comprising a pesticidally effective amount (i.e. an arthropodicidally effective amount, a nematocidally effective amount, an effective anti-helminth amount or an effective anti-protozoal amount) of a compound of formula (I) or (II) and an agriculturally acceptable inert carrier therefor. The expression "a compound of formula (I) or (II)" used here and throughout this application includes within its ambit the various stereoisomeric forms of the compounds of formulas (I) and (Π) and salts thereof.

In yet another aspect, the invention provides a method for controlling arthropod, nematode, helminths or protozoan pests at a locus, said method comprising applying to said locus a pesticidically effective amount (i.e. an arthropodicidally or nematocidally effective amount or an effective anti-helminth or anti-protozoal amount) of a compound of formula (I) or (II) or of a pesticidal composition as defined above.

Compounds of Formula (I) wherein X is O and R2 is not H are prepared from compounds of Formula (I) wherein X is an electron pair and R is not H said compounds of Formula (I) also being part of the invention] by oxidation of a sulfur atom into a sulfoximine group according to any method known per se by those skilled in the art. Such transformations can be made by various oxidizing reagents, including, but not limited to, potassium permanganate, sodium periodate and ruthenium tetroxide. This transformation 5 can take place in common solvents such as water, ethers e.g. dioxane, nitriles e.g. acetonitrile, or halohydrocarbons such as dichloromethane, chloroform, carbontetrachloride and the like, at temperatures between about -100°C and about 100°C, preferably between about 0°C and about 50°C. Such chemistry can be similar to that found in Tetrahedron, 1975,31, 505.

Compounds of Formula (I) in which X is an electron pair and R2 is other than H can be prepared from compounds of Formula (Π) by reaction of an appropriate electrophile R2-L in the presence of a base. R2 has the hereinabove-given meaning except that it is not H, and L is a leaving group. Examples of leaving groups L are halides, acetate, phenyl sulfonates, alkyl sulfonates and phenoxy groups. Examples of bases which can be used in the reaction are sodium hydride, triethylamine and potassium tert-butoxide.

Such reactions can take place in a variety of common solvents, such as, but not limited to, ethers such as tetrahydrofuran or dioxane; water; halohydrocarbons such as dichloromethane or chloroform; nitriles such as acetonitrile; and the like. Such reactions can take place at temperatures between about -100°C and about 100°C, but preferably between about 0°C and the boiling temperature of the solvent.

Compounds of Formula (I) in which X is an electron pair and in which R is H can be prepared from the corresponding compounds of Formula (I) in which R2 is an ester grouping COOR14, by conventional hydrolysis.

Compounds of Formula (II) can be prepared from compounds of Formula (III) by amination according to a reaction known per se to those skilled in the art. R, (ΠΙ)

Such chemistry can occur upon mixing a sulfide of Formula (ΠΙ) with an aminating reagent such as, but not limited to, an O-benzoylhydroxylamine, e.g. 0-(2,4,6-trimethylbenzoyl)hydroxylamine or 0-(3-chlorobenzoyl)hydroxylamine; an O-sulfonylhydroxylamines such as, but not limited to, hydroxylamine sulfonic acid or O-(2,4,6-triisopropylbenzenesulfonyl)hydroxylamine; or an O-phosphinic hydroxylamine, such as O-(diphenylphosphinyl)hydroxylamine. This can take place in a variety of solvents, including, but not limited to, water, halogenated hydrocarbons such as dichloromethane, chloroform, dichloroethane and the like, and aromatic solvents like benzene, toluene, xylenes and the like, and can take place at a temperature between about -100°C and about 100°C, 0°C 6 to the boiling point of the solvent being preferred. Such chemistry may be similar to that found in Aldrichimica Acta, 1980,13(1)3.

Compounds of Formula (I) wherein X is NH and R2 is H can be prepared from compounds of Formula (III) by reaction with chloramine [Tetrahedron, 1970, 51, 4449].

Such a reaction can take place in ammonia at a temperature between about -100°C and -33°C. 3 3

Compounds of Formula (I) wherein =X is =NR (wherein R is as defined above except that it is not hydrogen) and wherein R2 is H, can be derived from compounds of Formula (I) wherein =X is NH and R2 is H, by reaction of an appropriate electrophile R3-L in the presence of a base. R3 is as defined above except that it is not H, and L is a leaving group. Examples of leaving groups L are halides, acetate, phenyl sulfonates, alkyl sulfonates and phenoxy groups. Examples of bases which can be used in the reaction are sodium hydride, triethylamine and potassium tert-butoxide.

Such reactions can take place in a variety of common solvents, such as, but not limited to, ethers such as tetrahydrofuran or dioxane; water; halohydrocarbons such as dichloromethane or chloroform; nitriles such as acetonitrile; and the like. Such reactions can take place at temperatures between about -100°C and about 100°C, but preferably between about 0°C and the boiling temperature of the solvent. Similar reactions are found in Chem. Ber., 1984,117, 2779.

Compounds of Formula (I) wherein =X is =NR3 wherein R2 and R3 are the same and neither is hydrogen can be derived from compounds of Formula (I) wherein R is H and X is NH by reaction with at least two equivalents of an appropriate electrophile R -L in the presence of a base. R3 has the hereinabove-given meaning except that it is not H, and L is a leaving group. Examples of leaving groups L are halides, acetate, phenyl sulfonates, alkyl sulfonates and phenoxy groups. Examples of bases which can be used in the reaction are sodium hydride, triethylamine and potassium tert-butoxide.

Such reactions can take place in a variety of common solvents, such as, but not limited to, ethers such as tetrahydrofuran or dioxane; water; halohydrocarbons such as dichloromethane or chloroform; nitriles such as acetonitrile; and the like. Such reactions can take place at temperatures between about -100°C and about 100°C, but preferably between about 0°C and the boiling temperature of the solvent. Similar reactions are found in Lieb. Ann. Chem., 1972,759, 107.

Compounds of Formula (III) are known in the art. For example, those wherein Q is Q-l are described in European Patent Publication No 418016; European Patent Publication No 403309; U.S. Patent 5,104,994; European Patent Publication No 352944; U.S. Patent 5,079,370; U.S. Patent 5,047,550; U.S. Patent 5,232,940; U.S. Patent 4,810,720; U.S. Patent 5 4,804,675; U.S 5,306,694; U.S. Patent 4,614,533; WPO Publication No. 93/06089 and WPO Publication No. 94/21606. The compounds of Formula (III) wherein Q is Q-2 are described in U.S. Patent 5,187,185. Compounds of Formula (III) wherein Q is Q-3 are described in ί U.S. Patent 5,223,525.

In the many transformations hereinabove described, it is apparent that selected 10 substituents may occasionally interfere in the contemplated reactions. Such undesired effects can be avoided by using appropriate protecting groups to prevent the unwanted side reactions. It is also possible to use reagents that do not affect functional groups other than ' those desired to be changed. The particular choice of the appropriate protecting groups and reagents will be easily understood by those skilled in the art. The use of Chemical Abstracts 15 is considered and suggested as part of the knowledge of the person skilled in the art. ! j In order to further illustrate the present invention and the advantages thereof, the | following specific examples are given, it being understood that these examples are for the purpose of illustration only and in no way limit the scope of the invention. 8 EXAMPLE 1 2,4,6-Trimethylbenzenesulfonic acid, compound with S-4-[5-amino-3-cyano-l-(2,6-dichloro-4-trifluoromethyl)phenyl]pyrazolyl-S-ethylsulfilimine:

Ethyl O-mesitylene sulfonylacetohydroxamate (10 g, 0.035 mol) was dissolved in 5 dioxane (10 mL) and cooled to 0°C. 70% Perchloric acid (3.3 mL, 0.038 mol) was added and the mixture was stirred for 10 minutes. Water (200 mL) was added and the remaining solid was filtered, washed with water, then dissolved in methylene chloride (50 mL) and separated from the aqueous phase. 5-Amino-3-cyano-1 -(2,6-dichloro-4-trifluoromethyl)phenyl-4-ethylthiopyrazole (10.7 10 g, 0.028 mol) was dissolved in methylene chloride (50 mL) and the resulting solution was cooled to 0°C. The solution from above was added. After stirring for 1 hr at 0°C and then at room temperature, methylene chloride was removed and diethyl ether was added (200 mL). The resulting solid was filtered to provide the title compound as a white solid (12.45 g, 75%), m.p. about 193°C. 15 In a similar manner, the following were prepared: 2,4,6-Trimethylbenzene-sulfonic acid, compound with S-4-[5-amino-3-cyano-l-(2,6-dichloro-4-

trifluoromethyl)phenyl]pyrazolyl-S-methylsulfilimine, m.p. about 180°C hereinafter know as EXAMPLE la; 2,4,6-Trimethylbenzenesulfonic acid, compound with S-4-[5-amino-1-(2,6-dichloro-4-trifluoromethyl)phenyl]pyrazolyl-S-methylsulfilimine, m.p. about 187°C C 2 0 hereinafter know as EXAMPLE lb.

The following two compounds were also prepared by the above method, but were not isolated, but used as in EXAMPLE 2: 2,4,6-Trimethylbenzenesulfonic acid, compound with S-4-[5-amino-l-(2,6-dichloro-4-trifluoromethyl)phenyl-3-methyl]pyrazolyl-S- ethylsulfilimine and 2,4,6-Trimethylbenzenesulfonic acid, compound with S-4-[5-amino-l-25 (2,6-dichloro-4-trifluoromethyl)phenyl-3-ethyl]pyrazolyl-S-ethylsulfilimine. EXAMPLE 2 S-{[5-Amino-3-cyano-l-(2,6-dichloro-4-trifluoromethyl)phenyl]-4-(lH&gt;pyrazolyI)}&gt;S- ethyl-N-(tert-butoxycarbonyl)sulfilimine:

The product of EXAMPLE 1 (1.0 g, 1.7 mmol) was stirred in methylene chloride (10 5 mL), cooled to 0°C, and triethylamine (1.2 mL, 8.5 mmol) was added. Di-tert- butyldicarbonate (0.6 mL, 2.6 mmol) was added and the reaction was stirred 50 minutes.

The mixture was diluted with diethyl ether and washed with water (3 x 50 mL) and saturated aqueous sodium chloride solution (75 mL). The organic layer was dried, filtered and concentrated. The resulting oil was mixed with cold pentane and the precipitate was filtered. 10 The solid was recombined with the filtrate and solvent was removed and the oil filtered through silica gel using 2:3 ethyl acetate-.hexane as eluent. After removal of solvent, precipitation from diethyl ether/pentane provided the title compound as a white solid (0.36 g, 43%), m.p. about 191 °C.

In a similar manner, the following compounds were prepared (TABLE 1). 15 10 TABLE 1

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EXAMPLE # R1 R2 R7 m.p. 3 Et COMe CN about 163°C 4 Et COOMe CN about 200°C 5 Et SO2Me CN about 191°C 6 Et CONHMe CN about187°C 7 Et CN CN about175°C 8 Et CHO CN about181°C 9 Me COMe CN about159°C 10 Et PO(OEt)2 CN gum 11 Et CON(Me)2 CN about173°C 12 Et PO(Me)2 CN about150°C 13 Et CONHCOCC13 CN about116°C 14 Et conhcoch2ci CN about159°C 15 Et C(S)NHMe CN about 90°C 11 TABLE 1 (Continued)

EXAMPLE # R1 R2 R7 m.p. 16 Et CONHCH2COOEt CN about 91°C 17 Me C(S)NHMe CN about 95°C 18 Et CONHCOOEt CN about 167°C 19 Me CHO CN about160°C 20 Me CN CN about181°C 21 Me C(O)C(O)Me CN about 204°C 22 Me COO'Bu CN about196°C 23 Me CHO H about199°C 24 Me COMe H about181°C 25 Me CN H about182°C 26 Et CHO Me about159°C 27 Et CN Me about 67°C 28 Et CHO Et gum 29 Et CN Et about 64°C 12 EXAMPLE 30 N-(tert-Butoxycarbonyl)-S-4-[5-amino-3-cyano-l-(2,6-dichloro-4- trifluoromethyl)phenylpyrazolyl]-S-ethylsulfoximine:

The product of EXAMPLE 2 (1.55 g, 31 mmol) was dissolved in a 1:1 mixture of acetonitrilexarbon tetrachloride (19 mL). Sodium metaperiodate (2.7 g, 12.4 mmol) was added as a solution in water (19 mL). Ruthenium (III) chloride hydrate (20 mg; used to make the tetroxide in situ) and acetonitrile (25 mL) were added. After 2 hours, more sodium periodate (1.8 g, 8.2 mmol) and ruthenium (III) chloride hydrate (15 mg; forming the oxide in situ) were added and the reaction was stirred for 30 minutes. Then water (100 mL) and diethyl ether (100 mL) and isopropanol (2 mL) were successively added and mixed. Separation of the organic phase was followed by washes with water (100 mL) and saturated aqueous sodium chloride solution (100 mL). After drying over magnesium sulfate, the mixture was filtered and the solvent was removed to provide an oily residue which was triturated with cold diethyl ether and methylene chloride to provide the title compound as a brown, gummy solid (0.94 g, 60%). The proton nuclear magnetic resonance spectrum made in CDC13 has the following chemical shifts: 7.81 (m, 2H); 5.57 (brs, 2H); 3.7 - 3.5 (m, 2H); 1.44 (s, 9H); 1.39 (t, 3H).

In a similar manner, N-Acetyl-S-4-[5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethyl)phenylpyrazolyl]-S-ethylsulfoximine (m.p. about 217°C) was prepared, hereinafter known as EXAMPLE 30a. EXAMPLE 31 S-4-[5-Amino-3-cyano-l-(2,6-dichloro-4-trifluoromethyl)phenylpyrazolyl]-S- ethylsulfoximine:

The product of EXAMPLE 30 (0.1 g, 0.2 mmol) was dissolved in 2 mL of acetonitrile. Powdered molecular sieves (0.1 g), sodium iodide (0.07 g, 0.46 mmol) and chiorotrimethylsilane (0.06 mL, 0.46 mmol) were combined in 2 mL acetonitrile and the above solution added to it. After 25 minutes, the mixture was diluted with diethyl ether (7 mL) and sequentially washed with water, 10% aqueous hydrochloric acid solution and saturated aqueous sodium chloride solution. The organic phase was dried over sodium sulfate, filtered and concentrated under reduced pressure. The residual oil was triturated with cold pentane and dichloromethane to leave the desired product as a yellow solid (46 mg) having a melting point of about 86°C. 13 EXAMPLE 32 S-[5-Amino-3-cyano-l-(2,6-dichloro-4-trifluoromethyl)phenyl-4-(lH-pyrazolyl)]-S- methyl-N-[(4-methylphenyl)sulfonyl]sulfiIimine: 5 To a stirred solution of 5-amino-1-(2,6-dichloro-4-trifluoromethyl)phenyl-4- methylthio-lH-pyrazole-3-carbonitrile (0.99 g, 2.7 mmol) in acetonitrile (25 mL) was added an aqueous solution of N-chloro-p-toluenesulfonamide, sodium salt, hydrate (Chloramine-T hydrate) (0.61 g, 2.7 mmol) in water (5 mL), over a 2-minute interval. Stirring under ambient conditions was continued for approximately 2 hours and the mixture then heated to 10 boiling on a steam bath for 1 hour. Volatiles were removed under reduced pressure and the residue chromatographed on silica gel, eluting with 3:1 ethyl acetate/hexane, to give 0.81 g of the title compound as a solid having a melting point of about 197°C. 14 EXAMPLE 33 S-4-[5-Amino-3-cyano-l-(2-(3-chIoro-5-trifiuoromethyl)pyridyl)pyrazolyl]-S- ethylsulfoxide

Ethyl O-mesitylene sulfonylacetohydroxamate (0.47 g, 1.64 mmol) was dissolved in 5 dioxane (1 mL) and cooled to 0°C. 70% Perchloric acid (0.5 mL) was added and the mixture was stirred for 10 minutes. Water was added and the remaining solid was filtered, washed with water, then dissolved in methylene chloride and separated from the aqueous phase. 5-Amino-3-cyano-l-(2-(3-chloro-5-trifluoromethyl)pyridyl)-4-ethylsulfinylpyrazole (0.5 g, 1.37 mmol) was dissolved in methylene chloride (25 mL) and the resulting solution 10 was cooled to 0°C. The solution from above was added. After one month, the mixture was concentrated to a solid and washed repeatedly until no starting pyrazole remained. This provided the title compound as a white solid, m.p. around 193°C.

Further illustrative specific compounds of the invention are set forth below in 15 TABLES 2-5 below. Throughout these tables, the notation """ is used to indicate a lone electron pair. 15 TABLE 2

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R1 R7 R8 NR2 Me CN nh2 NCOEt Me CN nh2 NCOPr Me CN nh2 NCOiPr Me CN nh2 NCOtBu Me CN nh2 NCOPh Me CN nh2 NSO2Et Me CN nh2 NSO2Ph Me CN nh2 NSO2Pr Me CN nh2 NSO2iPr Me CN nh2 NNO2 Me CN nh2 NCOOEt Me CN nh2 NCOOPh 16 TABLE 2, Continued R1 R7 R8 NR2 Me CN NH2 NCOOPr Me CN nh2 NCOOiPr Me CN nh2 NCONHEt Me CN nh2 NCONHPr Me CN nh2 NCONHiPr Me CN nh2 NCOSMe Me CN nh2 NCOSEt Me CN nh2 NCSOMe Me CN nh2 NCSOEt Me CN nh2 NCSOPr Me CN nh2 NSO2NH2 Me CN nh2 NSO2NHMe Me CN nh2 NSO2NMe2 Me CN nh2 NP(O)(OMe)2 Me CN nh2 NP(O)(OMe)(OMe) Me CN nh2 NP(O)(OPr)2 Me CN nh2 NP(O)(Et)2 Me CN nh2 NC(O)C(O)H Me CN nh2 NC(O)C(O)Me Me CN nh2 NC(O)C(O)OMe Me CN nh2 NC(O)C(O)OEt Me CN nh2 NC(O)C(O)NH2 Me CN nh2 NC(O)C(O)OH Me CN nh2 NC(NH)NH2 17

Me CN nh2 NC(NOH)NH2 Me CN nh2 NC(NH)NHMe Me CN nh2 NC(NH)NMe2 Me CN nh2 NC(NH)OMe Me CN nh2 NC(NH)OEt Et CN nh2 NCOEt Et CN nh2 NCOPr Et CN nh2 NCOiPr Et CN nh2 NCOtBu Et CN nh2 NCOPh Et CN nh2 NSO2Et Et CN nh2 NSO2Ph Et CN nh2 NSO2Pr Et CN nh2 NSO2iPr Et CN nh2 nno2 Et CN nh2 NCOOEt Et CN nh2 NCOOPh Et CN nh2 NCOOPr Et CN nh2 NCOOiPr Et CN nh2 NCONHEt Et CN nh2 NCONHPr Et CN nh2 NCONHiPr Et CN nh2 NCOSMe Et CN nh2 NCOSEt Et CN nh2 NCSOMe Et CN nh2 NCSOEt Et CN nh2 NCSOPr Et CN nh2 NSO2NH2 18

Et CN nh2 NSO2NHMe Et CN nh2 NSO2NMe2 Et CN nh2 NP(O)(OMe)2 Et CN nh2 NP(O)(OMe)(OMe) Et CN nh2 NP(O)(OPr)2 Et CN nh2 NP(O)(Et)2 Et CN nh2 NC(O)C(O)H Et CN nh2 NC(O)C(O)Me Et CN nh2 NC(O)C(O)OMe Et CN nh2 NC(O)C(O)OEt Et CN nh2 NC(O)C(O)NH2 Et CN nh2 NC(O)C(O)OH Et CN nh2 NC(NH)NH2 Et CN nh2 NC(NOH)NH2 Et CN nh2 NC(NH)NHMe Et CN nh2 NC(NH)NMe2 Et CN nh2 NC(NH)OMe Et CN nh2 NC(NH)OEt Me CN NHMe NCOMe Me CN NHMe NCOEt Me CN NHMe NCOPr Me CN NHMe NCHO Me CN NHMe NCOiPr Me CN NHMe NCOtBu Me CN NHMe NCOPh Me CN NHMe NSO2Me Me CN NHMe NSO2Et Me CN NHMe NSO2Pr 19

Me CN NHMe NSO2Ph Me CN NHMe NSO2iPr Me CN NHMe NNO2 Me CN NHMe NCOOMe Me CN NHMe NCOOEt Me CN NHMe NCOOPr Me CN NHMe NCOOiPr Me CN NHMe NCONHEt Me CN NHMe NCONHPr Me CN NHMe nconh2 Me CN NHMe NCONHMe Me CN NHMe NCN Me CN NHMe NCOSMe Me CN NHMe NCOSEt Me CN NHMe NCSOMe Me CN NHMe NCSOEt Me CN NHMe NCSOPr Me CN NHMe nso2nh2 Me CN NHMe NSO2NHMe Me CN NHMe NSO2NMe2 Me CN NHMe NP(O)(OMe)2 Me CN NHMe NP(O)(OEt)2 Me CN NHMe NP(O)Me2 Me CN NHMe NP(O)Et2 Me CN NHMe NP(O)Me(OMe) Me CN NHMe NP(O)(OPr)2 Me CN NHMe NC(O)C(O)H Me CN NHMe NC(O)C(O)Me 20

Me CN NHMe NC(O)C(O)OMe Me CN NHMe NC(0)C(0)0Et Me CN NHMe NC(0)C(0)NH2 Me CN NHMe NC(O)C(O)OH Me CN NHMe NC(NH)NH2 Me CN NHMe NC(NOH)NH2 Me CN NHMe NC(NH)NHMe Me CN NHMe NC(NH)NMe2 Me CN NHMe NC(NH)OMe Me CN NHMe NC(NH)OEt Me CN NHEt NCOMe Me CN NHEt NCOEt Me CN NHEt NCOPr Me CN NHEt NCHO Me CN NHEt NCOiPr Me CN NHEt NCOtBu Me CN NHEt NCOPh Me CN NHEt NSO2Me Me CN NHEt NSO2Et Me CN NHEt NSO2Pr Me CN NHEt NSO2Ph Me CN NHEt NSO2iPr Me CN NHEt NN02 Me CN NHEt NCOOMe Me CN NHEt NCOOEt Me CN NHEt NCOOPr Me CN NHEt NCOOiPr Me CN NHEt NCONHEt 21

Me CN NHEt NCONHPr Me CN NHEt nconh2 Me CN NHEt NCONHMe Me CN NHEt NCN Me CN NHEt NCOSMe Me CN NHEt NCOSEt Me CN NHEt NCSOMe Me CN NHEt NCSOEt Me CN NHEt NCSOPr Me CN NHEt NSO2NH2 Me CN NHEt NSO2NHMe Me CN NHEt NSO2NMe2 Me CN NHEt NP(O)(OMe)2 Me CN NHEt NP(O)(OEt)2 Me CN NHEt NP(O)Me2 Me CN NHEt NP(O)Et2 Me CN NHEt NP(O)Me(OMe) Me CN NHEt NP(O)(OPr)2 Me CN NHEt NC(O)C(O)H Me CN NHEt NC(O)C(O)Me Me CN NHEt NC(O)C(O)OMe Me CN NHEt NC(O)C(O)OEt Me CN NHEt NC(O)C(O)NH2 Me CN NHEt NC(O)C(O)OH Me CN NHEt NC(NH)NH2 Me CN NHEt NC(NOH)NH2 Me CN NHEt NC(NH)NHMe Me CN NHEt NC(NH)NMe2 22

Me CN NHEt NC(NH)OMe Me CN NHEt NC(NH)OEt Me CN NHPr NCOMe Me CN NHPr NCOEt Me CN NHPr NCOPr Me CN NHPr NCHO Me CN NHPr NCOiPr Me CN NHPr NCOtBu Me CN NHPr NCOPh Me CN NHPr NSO2Me Me CN NHPr NSO2Et Me CN NHPr NSO2Pr Me CN NHPr NSO2Ph Me CN NHPr NSO2iPr Me CN NHPr NNO2 Me CN NHPr NCOOMe Me CN NHPr NCOOEt Me CN NHPr NCOOPr Me CN NHPr NCOOiPr Me CN NHPr NCONHEt Me CN NHPr NCONHPr Me CN NHPr nconh2 Me CN NHPr NCONHMe Me CN NHPr NCN Me CN NHPr NCOSMe Me CN NHPr NCOSEt Me CN NHPr NCSOMe Me CN NHPr NCSOEt 23

Me CN NHPr NCSOPr Me CN NHPr nso2nh2 Me CN NHPr NSO2NHMe Me CN NHPr NSO2NMe2 Me CN NHPr NP(O)(OMe)2 Me CN NHPr NP(O)(OEt)2 Me CN NHPr NP(O)Me2 Me CN NHPr NP(O)Et2 Me CN NHPr NP(O)Me(OMe) Me CN NHPr NP(O)(OPr)2 Me CN NHPr NC(O)C(O)H Me CN NHPr NC(O)C(O)Me Me CN NHPr NC(O)C(O)OMe Me CN NHPr NC(O)C(O)OEt Me CN NHPr NC(O)C(O)NH2 Me CN NHPr NC(O)C(O)OH Me CN NHPr NC(NH)NH2 Me CN NHPr NC(NOH)NH2 Me CN NHPr NC(NH)NHMe Me CN NHPr NC(NH)NMe2 Me CN NHPr NC(NH)OMe Me CN NHPr NC(NH)OEt Et CN NHMe NCOMe Et CN NHMe NCOEt Et CN NHMe NCOPr Et CN NHMe NCHO Et CN NHMe NCOiPr Et CN NHMe NCOtBu 24

Et CN NHMe NCOPh Et CN NHMe NSO2Me Et CN NHMe NSO2Et Et CN NHMe NSO2Pr Et CN NHMe NSO2Ph Et CN NHMe NSO2iPr Et CN NHMe nno2 Et CN NHMe NCOOMe Et CN NHMe NCOOEt Et CN NHMe NCOOPr Et CN NHMe NCOOiPr Et CN NHMe NCONHEt Et CN NHMe NCONHPr Et CN NHMe nconh2 Et CN NHMe NCONHMe Et CN NHMe NCN Et CN NHMe NCOSMe Et CN NHMe NCOSEt Et CN NHMe NCSOMe Et CN NHMe NCSOEt Et CN NHMe NCSOPr Et CN NHMe NSO2NH2 Et CN NHMe NSO2NHMe Et CN NHMe NSO2NMe2 Et CN NHMe NP(O)(OMe)2 Et CN NHMe NP(O)(OEt)2 Et CN NHMe NP(O)Me2 Et CN NHMe NP(O)Et2 25

Et CN NHMe NP(O)Me(OMe) Et CN NHMe NP(O)(OPr)2 Et CN NHMe NC(O)C(O)H Et CN NHMe NC(O)C(O)Me Et CN NHMe NC(O)C(O)OMe Et CN NHMe NC(O)C(O)OEt Et CN NHMe NC(O)C(O)NH2 Et CN NHMe NC(O)C(O)OH Et CN NHMe NC(NH)NH2 Et CN NHMe NC(NOH)NH2 Et CN NHMe NC(NH)NHMe Et CN NHMe NC(NH)NMe2 Et CN NHMe NC(NH)OMe Et CN NHMe NC(NH)OEt Et CN NHEt NCOMe Et CN NHEt NCOEt Et CN NHEt NCOPr Et CN NHEt NCHO Et CN NHEt NCOiPr Et CN NHEt NCOtBu Et CN NHEt NCOPh Et CN NHEt NSO2Me Et CN NHEt NSO2Et Et CN NHEt NSO2Pr Et CN NHEt NSO2Ph Et CN NHEt NSO2iPr Et CN NHEt nno2 Et CN NHEt NCOOMe 26

Et CN NHEt NCOOEt Et CN NHEt NCOOPr Et CN NHEt NCOOiPr Et CN NHEt NCONHEt Et CN NHEt NCONHPr Et CN NHEt NCONH2 Et CN NHEt NCONHMe Et CN NHEt NCN Et CN NHEt NCOSMe Et CN NHEt NCOSEt Et CN NHEt NCSOMe Et CN NHEt NCSOEt Et CN NHEt NCSOPr Et CN NHEt NSO2NH2 Et CN NHEt NSO2NHMe Et CN NHEt NSO2NMe2 Et CN NHEt NP(O)(OMe)2 Et CN NHEt NP(O)(OEt)2 Et CN NHEt NP(O)Me2 Et CN NHEt NP(O)Et2 Et CN NHEt NP(O)Me(OMe) Et CN NHEt NP(O)(OPr)2 Et CN NHEt NC(O)C(O)H Et CN NHEt NC(O)C(O)Me Et CN NHEt NC(O)C(O)OMe Et CN NHEt NC(O)C(O)OEt Et CN NHEt NC(O)C(O)NH2 Et CN NHEt NC(O)C(O)OH 27

Et CN NHEt NC(NH)NH2 -Et CN NHEt NC(NOH)NH2 Et CN NHEt NC(NH)NHMe Et CN NHEt NC(NH)NMe2 Et CN NHEt NC(NH)OMe Et CN NHEt NC(NH)OEt Et CN NHPr NCOMe Et CN NHPr NCOEt Et CN NHPr NCOPr Et CN NHPr NCHO Et CN NHPr NCOiPr Et CN NHPr NCOtBu Et CN NHPr NCOPh Et CN NHPr NSO2Me Et CN NHPr NSO2Et Et CN NHPr NSO2Pr Et CN NHPr NSO2Ph Et CN NHPr NSO2iPr Et CN NHPr nno2 Et CN NHPr NCOOMe Et CN NHPr NCOOEt Et CN NHPr NCOOPr Et CN NHPr NCOOiPr Et CN NHPr NCONHEt Et CN NHPr NCONHPr Et CN NHPr nconh2 Et CN NHPr NCONHMe Et CN NHPr NCN 28

Et CN NHPr NCOSMe Et CN NHPr NCOSEt Et CN NHPr NCSOMe Et CN NHPr NCSOEt Et CN NHPr NCSOPr Et CN NHPr NSO2NH2 Et CN NHPr . NSO2NHMe Et CN NHPr NSO2NMe2 Et CN NHPr NP(O)(OMe)2 Et CN NHPr NP(O)(OEt)2 Et CN NHPr NP(O)Me2 Et CN NHPr NP(O)Et2 Et CN NHPr NP(O)Me(OMe) Et CN NHPr NP(O)(OPr)2 Et CN NHPr NC(O)C(O)H Et CN NHPr NC(O)C(O)Me Et CN NHPr NC(O)C(O)OMe Et CN NHPr NC(O)C(O)OEt Et CN NHPr NC(O)C(O)NH2 Et CN NHPr NC(O)C(O)OH Et CN NHPr NC(NH)NH2 Et CN NHPr NC(NOH)NH2 Et CN NHPr NC(NH)NHMe Et CN NHPr NC(NH)NMe2 Et CN NHPr NC(NH)OMe Et CN NHPr NC(NH)OEt Me CN nh2 NCOMe Me CN nh2 NCOEt 29

Me CN nh2 NCOPr 0 Me CN nh2 NCHO 0 Me CN nh2 NCOiPr 0 Me CN nh2 NCOtBu 0 Me CN nh2 NCOPh 0 Me CN nh2 NSO2Me 0 Me CN nh2 NSO2Et 0 Me CN nh2 NSO2Pr o Me CN nh2 NSO2Ph 0 Me CN nh2 NSO2iPr 0 Me CN nh2 NNO2 0 Me CN nh2 NCOOMe 0 Me CN nh2 NCOOEt 0 Me CN nh2 NCOOPr 0 Me CN nh2 NCOOiPr 0 Me CN nh2 NCONHEt 0 Me CN nh2 NCONHPr o Me CN nh2 NCONH2 0 Me CN nh2 NCONHMe 0 Me CN nh2 NCN 0 Me CN nh2 NCOSMe o Me CN nh2 NCOSEt 0 Me CN nh2 NCSOMe 0 Me CN nh2 NCSOEt 0 Me CN nh2 NCSOPr 0 Me CN nh2 NSO2NH2 0 Me CN nh2 NSO2NHMe 0 Me CN nh2 NSO2NMe2 0 30

Me CN nh2 NP(O)(OMe)2 0 Me CN nh2 NP(O)(OEt)2 0 Me CN nh2 NP(O)Me2 O Me CN nh2 NP(O)Et2 O Me CN nh2 NP(O)Me(OMe) 0 Me CN nh2 NP(O)(OPr)2 0 Me CN nh2 NC(O)C(O)H O Me CN nh2 NC(O)C(O)Me 0 Me CN nh2 NC(O)C(O)OMe 0 Me CN nh2 NC(O)C(O)OEt 0 Me CN nh2 NC(O)C(O)NH2 0 Me CN nh2 NC(O)C(O)OH 0 Me CN nh2 NC(NH)NH2 0 Me CN nh2 NC(NOH)NH2 0 Me CN nh2 NC(NH)NHMe 0 Me CN nh2 NC(NH)NMe2 0 Me CN nh2 NC(NH)OMe O Me CN nh2 NC(NH)OEt 0 Me CN nh2 NH 0 Me CN NHMe NCOMe 0 Me CN NHMe NCOEt 0 Me CN NHMe NCOPr 0 Me CN NHMe NCHO 0 Me CN NHMe NCOiPr 0 Me CN NHMe NCOtBu 0 Me CN NHMe NCOPh 0 Me CN NHMe NSO2Me 0 Me CN NHMe NSO2Et 0 31

Me CN NHMe NSOiPr 0 Me CN NHMe NSO2Ph O Me CN NHMe NSOoiPr 0 Me CN NHMe nno2 0 Me CN NHMe NCOOMe 0 Me CN NHMe NCOOEt 0 Me CN NHMe NCOOPr 0 Me CN NHMe NCOOiPr 0 Me CN NHMe NCONHEt 0 Me CN NHMe NCONHPr 0 Me CN NHMe NCONH2 0 Me CN NHMe NCONHMe 0 Me CN NHMe NCN 0 Me CN NHMe NCOSMe 0 Me CN NHMe NCOSEt 0 Me CN NHMe NCSOMe 0 Me CN NHMe NCSOEt 0 Me CN NHMe NCSOPr 0 Me CN NHMe NSO2NH2 0 Me CN NHMe NSO2NHMe 0 Me CN NHMe NSO2NMe2 0 Me CN NHMe NP(O)(OMe)2 0 Me CN NHMe NP(O)(OEt)2 0 Me CN NHMe NP(O)Me2 0 Me CN NHMe NP(O)Et2 0 Me CN NHMe NP(O)Me(OMe) o Me CN NHMe NP(O)(OPr)2 0 Me CN NHMe NC(O)C(O)H 0 32

Me CN NHMe NC(O)C(O)Me 0 Me CN NHMe NC(O)C(O)OMe 0 Me CN NHMe NC(O)C(O)OEt 0 Me CN NHMe NC(O)C(O)NH2 O Me CN NHMe NC(O)C(O)OH 0 Me CN NHMe NC(NH)NH2 0 Me CN NHMe NC(NOH)NH2 0 Me CN NHMe NC(NH)NHMe O Me CN NHMe NC(NH)NMe2 0 Me CN NHMe NC(NH)OMe O Me CN NHMe NC(NH)OEt 0 Me CN NHEt NCOMe 0 Me CN NHEt NCOEt 0 Me CN NHEt NCOPr 0 Me CN NHEt NCHO 0 Me CN NHEt NCOiPr 0 Me CN NHEt NCOtBu 0 Me CN NHEt NCOPh O Me CN NHEt NSO2Me 0 Me CN NHEt NSO2Et 0 Me CN NHEt NSO2Pr 0 Me CN NHEt NSO2Ph 0 Me CN NHEt NSO2iPr 0 Me CN NHEt NNO2 0 Me CN NHEt NCOOMe o Me CN NHEt NCOOEt 0 Me CN NHEt NCOOPr 0 Me CN NHEt NCOOiPr 0 33

Me CN NHEt NCONHEt O Me CN NHEt NCONHPr 0 Me CN NHEt NCONH2 0 Me CN NHEt NCONHMe 0 Me CN NHEt NCN 0 Me CN NHEt NCOSMe 0 Me CN NHEt NCOSEt 0 Me CN NHEt NCSOMe 0 Me CN NHEt NCSOEt 0 Me CN NHEt NCSOPr 0 Me CN NHEt NSO2NH2 0 Me CN NHEt NSO2NHMe 0 Me CN NHEt NSO2NMe2 0 Me CN NHEt NP(O)(OMe)2 0 Me CN NHEt NP(O)(OEt)2 0 Me CN NHEt NP(O)Me2 0 Me CN NHEt NP(O)Et2 0 Me CN NHEt NP(O)Me(OMe) 0 Me CN NHEt NP(O)(OPr)2 0 Me CN NHEt NC(O)C(O)H 0 Me CN NHEt NC(O)C(O)Me 0 Me CN NHEt NC(O)C(O)OMe 0 Me CN NHEt NC(O)C(O)OEt 0 Me CN NHEt NC(O)C(O)NH2 0 Me CN NHEt NC(O)C(O)OH 0 Me CN NHEt NC(NH)NH2 0 Me CN NHEt NC(NOH)NH2 0 Me CN NHEt NC(NH)NHMe 0 34

Me CN NHEt NC(NH)NMe2 0 Me CN NHEt NC(NH)OMe 0 Me CN NHEt NC(NH)OEt 0 Et CN nh2 NCOEt 0 Et CN nh2 NCOPr 0 Et CN nh2 NCHO 0 Et CN nh2 NCOiPr 0 Et CN nh2 NCOtBu 0 Et CN nh2 NCOPh 0 Et CN nh2 NSO2Me 0 Et CN nh2 NSO2Et 0 Et CN nh2 NSO2Pr 0 Et CN nh2 NSO2Ph 0 Et CN nh2 NSO2iPr 0 Et CN nh2 NNO2 0 Et CN nh2 NCOOMe 0 Et CN nh2 NCOOEt 0 Et CN nh2 NCOOPr 0 Et CN nh2 NCOOiPr 0 Et CN nh2 NCONHEt 0 Et CN nh2 NCONHPr 0 Et CN nh2 nconh2 0 Et CN nh2 NCONHMe 0 Et CN nh2 NCN 0 Et CN nh2 NCOSMe 0 Et CN nh2 NCOSEt 0 Et CN nh2 NCSOMe 0 Et CN nh2 NCSOEt 0 35

Et CN nh2 NCSOPr 0 Et CN nh2 NSO2NH2 0 Et CN nh2 NSO2NHMe 0 Et CN nh2 NSO2NMe2 0 Et CN nh2 NP(O)(OMe)2 O Et CN nh2 NP(O)(OEt)2 O Et CN nh2 NP(O)Me2 0 Et CN nh2 NP(O)Et2 O Et CN nh2 NP(O)Me(OMe) 0 Et CN nh2 NP(O)(OPr)2 0 Et CN nh2 NC(O)C(O)H 0 Et CN nh2 NC(O)C(O)Me 0 Et CN nh2 NC(O)C(O)OMe 0 Et CN nh2 NC(O)C(O)OEt 0 Et CN nh2 NC(O)C(O)NH2 0 Et CN nh2 NC(O)C(O)OH 0 Et CN nh2 NC(NH)NH2 0 Et CN nh2 NC(NOH)NH2 0 Et CN nh2 NC(NH)NHMe 0 Et CN nh2 NC(NH)NMe2 0 Et CN nh2 NC(NH)OMe 0 Et CN nh2 NC(NH)OEt 0 Et CN NHMe NH 0 Et CN NHMe NCOMe 0 Et CN NHMe NCOEt 0 Et CN NHMe NCOPr 0 Et CN NHMe NCHO 0 Et CN NHMe NCOiPr 0 36

Et CN NHMe NCOtBu 0 Et CN NHMe NCOPh 0 Et CN NHMe NSO2Me 0 Et CN NHMe NSO2Et 0 Et CN NHMe NSO2Pr 0 Et CN NHMe NSO2Ph 0 Et CN NHMe NSO2iPr 0 Et CN NHMe nno2 0 Et CN NHMe NCOOMe 0 Et CN NHMe NCOOEt 0 Et CN NHMe NCOOPr 0 Et CN NHMe NCOOiPr 0 Et CN NHMe NCONHEt 0 Et CN NHMe NCONHPr 0 Et CN NHMe NCONH2 0 Et CN NHMe NCONHMe 0 Et CN NHMe NCN 0 Et CN NHMe NCOSMe 0 Et CN NHMe NCOSEt 0 Et CN NHMe NCSOMe 0 Et CN NHMe NCSOEt 0 Et CN NHMe NCSOPr 0 Et CN NHMe NSO2NH2 0 Et CN NHMe NSO2NHMe 0 Et CN NHMe NSO2NMe2 0 Et CN NHMe NP(O)(OMe)2 0 Et CN NHMe NP(O)(OEt)2 0 Et CN NHMe NP(O)Me2 0 37

Et CN NHMe NP(O)Et2 Et CN NHMe NP(O)Me(OMe) Et CN NHMe NP(O)(OPr)2 Et CN NHMe NC(O)C(O)H Et CN NHMe NC(O)C(O)Me Et CN NHMe NC(O)C(O)OMe Et CN NHMe NC(O)C(O)OEt Et CN NHMe NC(O)C(O)NH2 Et CN NHMe NC(O)C(O)OH Et CN NHMe NC(NH)NH2 Et CN NHMe NC(NOH)NH2 Et CN NHMe NC(NH)NHMe Et CN NHMe NC(NH)NMe2 Et CN NHMe NC(NH)OMe Et CN NHMe NC(NH)OEt Et CN NHEt NCOMe Et CN NHEt NCOEt Et CN NHEt NCOPr Et CN NHEt NCHO Et CN NHEt NCOiPr Et CN NHEt NCOtBu Et CN NHEt NCOPh Et CN NHEt NSO2Me Et CN NHEt NSO2Et Et CN NHEt NSO2Pr Et CN NHEt NSO2Ph Et CN NHEt NSO2iPr Et CN NHEt nno2 Ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο 38

Et CN NHEt NCOOMe 0 Et CN NHEt NCOOEt 0 Et CN NHEt NCOOPr 0 Et CN NHEt NCOOiPr 0 Et CN NHEt NCONHEt 0 Et CN NHEt NCONHPr 0 Et CN NHEt NCONH2 0 Et CN NHEt NCONHMe 0 Et CN NHEt NCN 0 Et CN NHEt NCOSMe 0 Et CN NHEt NCOSEt 0 Et CN NHEt NCSOMe 0 Et CN NHEt NCSOEt 0 Et CN NHEt NCSOPr 0 Et CN NHEt NSO2NH2 0 Et CN NHEt NSO2NHMe 0 Et CN NHEt NSO2NMe2 0 Et CN NHEt NP(O)(OMe)2 0 Et CN NHEt NP(O)(OEt)2 0 Et CN NHEt NP(O)Me2 0 Et CN NHEt NP(O)Et2 0 Et CN NHEt NP(O)Me(OMe) 0 Et CN NHEt NP(O)(OPr)2 0 Et CN NHEt NC(O)C(O)H 0 Et CN NHEt NC(O)C(O)Me 0 Et CN NHEt NC(O)C(O)OMe 0 Et CN NHEt NC(O)C(O)OEt 0 Et CN NHEt NC(O)C(O)NH2 0 39

Et CN NHEt NC(O)C(O)OH 0 Et CN NHEt NC(NH)NH2 0 Et CN NHEt NC(NOH)NH2 0 Et CN NHEt NC(NH)NHMe 0 Et CN NHEt NC(NH)NMe2 0 Et CN NHEt NC(NH)OMe 0 Et CN NHEt NC(NH)OEt 0 Me CN NHCOMe NCOMe Me CN NHCOMe NCOEt Me CN NHCOMe NCOPr Me CN NHCOMe NCHO Me - CN NHCOMe NCOiPr Me CN NHCOMe NCOtBu Me CN NHCOMe NCOPh Me CN NHCOMe NSO2Me Me CN NHCOMe NSO2Et Me CN NHCOMe NSO2Pr Me CN NHCOMe NSO2Ph Me CN NHCOMe NSO2iPr Me CN NHCOMe nno2 Me CN NHCOMe NCOOMe Me CN NHCOMe NCOOEt Me CN NHCOMe NCOOPr Me CN NHCOMe NCOOiPr Me CN NHCOMe NCONHEt Me CN NHCOMe NCONHPr Me CN NHCOMe nconh2 Me CN NHCOMe NCONHMe 40

Me CN NHCOMe NCN Me CN NHCOMe NCOSMe Me CN NHCOMe NCOSEt Me CN NHCOMe NCSOMe Me CN NHCOMe NCSOEt Me CN NHCOMe NCSOPr Me CN NHCOMe NSO2NH2 Me CN NHCOMe NSO2NHMe Me CN NHCOMe NSO2NMe2 Me CN NHCOMe NP(O)(OMe)2 Me CN NHCOMe NP(O)(OEt)2 Me CN NHCOMe NP(O)Me2 Me CN NHCOMe NP(O)Et2 Me CN NHCOMe NP(O)Me(OMe) Me CN NHCOMe NP(O)(OPr)2 Me CN NHCOMe NC(O)C(O)H Me CN NHCOMe NC(O)C(O)Me Me CN NHCOMe NC(O)C(O)OMe Me CN NHCOMe NC(O)C(O)OEt Me CN NHCOMe NC(O)C(O)NH2 Me CN NHCOMe NC(O)C(O)OH Me CN NHCOMe NC(NH)NH2 Me CN NHCOMe NC(NOH)NH2 Me CN NHCOMe NC(NH)NHMe Me CN NHCOMe NC(NH)NMe2 Me CN NHCOMe NC(NH)OMe Me CN NHCOMe NC(NH)OEt Et CN NHCOMe NCOMe 41

Et CN NHCOMe NCOEt Et CN NHCOMe NCOPr Et CN NHCOMe NCHO Et CN NHCOMe NCOiPr Et CN NHCOMe NCOtBu Et CN NHCOMe NCOPh Et CN NHCOMe NSO2Me Et CN NHCOMe NSO2Et Et CN NHCOMe NSO2Pr Et CN NHCOMe NSO2Ph Et CN NHCOMe NSO2iPr Et CN NHCOMe nno2 Et CN NHCOMe NCOOMe Et CN NHCOMe NCOOEt Et CN NHCOMe NCOOPr Et CN NHCOMe NCOOiPr Et CN NHCOMe NCONHEt Et CN NHCOMe NCONHPr Et CN NHCOMe nconh2 Et CN NHCOMe NCONHMe Et CN NHCOMe NCN Et CN NHCOMe NCOSMe Et CN NHCOMe NCOSEt Et CN NHCOMe NCSOMe Et CN NHCOMe NCSOEt Et CN NHCOMe NCSOPr Et CN NHCOMe NSO2NH2 Et CN NHCOMe NSO2NHMe 42

Et CN NHCOMe NSO2NMe2 Et CN NHCOMe NP(O)(OMe)2 Et CN NHCOMe NP(O)(OEt)2 Et CN NHCOMe NP(O)Me2 Et CN NHCOMe NP(O)Et2 Et CN NHCOMe NP(O)Me(OMe) Et CN NHCOMe NP(O)(OPr)2 Et CN NHCOMe NC(O)C(O)H Et CN NHCOMe NC(O)C(O)Me Et CN NHCOMe NC(O)C(O)OMe Et CN NHCOMe NC(O)C(O)OEt Et CN NHCOMe NC(O)C(O)NH2 Et CN NHCOMe NC(O)C(O)OH Et CN NHCOMe NC(NH)NH2 Et CN NHCOMe NC(NOH)NH2 Et CN NHCOMe NC(NH)NHMe Et CN NHCOMe NC(NH)NMe2 Et CN NHCOMe NC(NH)OMe Et CN NHCOMe NC(NH)OEt Me CN NHCOOMe NCOMe Me CN NHCOOMe NCOEt Me CN NHCOOMe NCOPr Me CN NHCOOMe NCHO Me CN NHCOOMe NCOiPr Me CN NHCOOMe NCOtBu Me CN NHCOOMe NCOPh Me CN NHCOOMe NSO2Me Me CN NHCOOMe NSO2Et 43

Me CN NHCOOMe NSO2Pr Me CN NHCOOMe NSO2Ph Me CN NHCOOMe NSO2iPr Me CN NHCOOMe NNO2 Me CN NHCOOMe NCOOMe Me CN NHCOOMe NCOOEt Me CN NHCOOMe NCOOPr Me CN NHCOOMe NCOOiPr Me CN NHCOOMe NCONHEt Me CN NHCOOMe NCONHPr Me CN NHCOOMe NCONH2 Me CN NHCOOMe NCONHMe Me CN NHCOOMe NCN Me CN NHCOOMe NCOSMe Me CN NHCOOMe NCOSEt Me CN NHCOOMe NCSOMe Me CN NHCOOMe NCSOEt Me CN NHCOOMe NCSOPr Me CN NHCOOMe NSO2NH2 Me CN NHCOOMe NSO2NHMe Me CN NHCOOMe NSO2NMe2 Me CN NHCOOMe NP(O)(OMe)2 Me CN NHCOOMe NP(O)(OEt)2 Me CN NHCOOMe NP(O)Me2 Me CN NHCOOMe NP(O)Et2 Me CN NHCOOMe NP(O)Me(OMe) Me CN NHCOOMe NP(O)(OPr)2 Me CN NHCOOMe NC(O)C(O)H

I 44

Me CN NHCOOMe NC(O)C(O)Me Me CN NHCOOMe NC(O)C(O)OMe Me CN NHCOOMe NC(O)C(O)OEt Me CN NHCOOMe NC(O)C(O)NH2 Me CN NHCOOMe NC(O)C(O)OH Me CN NHCOOMe NC(NH)NH2 Me CN NHCOOMe NC(NOH)NH2 Me CN NHCOOMe NC(NH)NHMe Me CN NHCOOMe NC(NH)NMe2 Me CN. NHCOOMe NC(NH)OMe Me CN NHCOOMe NC(NH)OEt Et CN NHCOOMe NCOMe Et CN NHCOOMe NCOEt Et CN NHCOOMe NCOPr Et CN NHCOOMe NCHO Et CN NHCOOMe NCOiPr Et CN NHCOOMe NCOtBu Et CN NHCOOMe NCOPh Et CN NHCOOMe NSO2Me Et CN NHCOOMe NSO2Et Et CN NHCOOMe NSO2Pr Et CN NHCOOMe NSO2Ph Et CN NHCOOMe NSO2iPr Et CN NHCOOMe nno2 Et CN NHCOOMe NCOOMe Et CN NHCOOMe NCOOEt Et CN NHCOOMe NCOOPr Et CN NHCOOMe NCOOiPr 45

Et CN NHCOOMe NCONHEt Et CN NHCOOMe NCONHPr Et CN NHCOOMe nconh2 Et CN NHCOOMe NCONHMe Et CN NHCOOMe NCN Et CN NHCOOMe NCOSMe Et CN NHCOOMe NCOSEt Et CN NHCOOMe NCSOMe Et CN NHCOOMe NCSOEt Et CN NHCOOMe NCSOPr Et CN NHCOOMe nso2nh2 Et CN NHCOOMe NSO2NHMe Et CN NHCOOMe NSO2NMe2 Et CN NHCOOMe NP(O)(OMe)2 Et CN NHCOOMe NP(O)(OEt)2 Et CN NHCOOMe NP(O)Me2 Et CN NHCOOMe NP(O)Et2 Et CN NHCOOMe NP(O)Me(OMe) Et CN NHCOOMe NP(O)(OPr)2 Et CN NHCOOMe NC(O)C(O)H Et CN NHCOOMe NC(O)C(O)Me Et CN NHCOOMe NC(O)C(O)OMe Et CN NHCOOMe NC(O)C(O)OEt Et CN NHCOOMe NC(O)C(O)NH2 Et CN NHCOOMe NC(O)C(O)OH Et CN NHCOOMe NC(NH)NH2 Et CN NHCOOMe NC(NOH)NH2 Et CN NHCOOMe NC(NH)NHMe 46

Et CN NHCOOMe NC(NH)NMe2 Et CN NHCOOMe NC(NH)OMe Et CN NHCOOMe NC(NH)OEt Me CN NHCOOEt NCOMe Me CN NHCOOEt NCOEt Me CN NHCOOEt NCOPr Me CN NHCOOEt NCHO Me CN NHCOOEt NCOiPr Me CN NHCOOEt NCOtBu Me CN NHCOOEt NCOPh Me CN NHCOOEt NSO2Me Me CN NHCOOEt NSO2Et Me CN NHCOOEt NSO2Pr Me CN NHCOOEt NSO2Ph Me CN NHCOOEt NSO2iPr Me CN NHCOOEt NNO2 Me CN NHCOOEt NCOOMe Me CN NHCOOEt NCOOEt Me CN NHCOOEt NCOOPr Me CN NHCOOEt NCOOiPr Me CN NHCOOEt NCONHEt Me CN NHCOOEt NCONHPr Me CN NHCOOEt NCONH2 Me CN NHCOOEt NCONHMe Me CN NHCOOEt NCN Me CN NHCOOEt NCOSMe Me CN NHCOOEt NCOSEt Me CN NHCOOEt NCSOMe 47

Me CN NHCOOEt NCSOEt Me CN NHCOOEt NCSOPr Me CN NHCOOEt nso2nh2 Me CN NHCOOEt NSO2NHMe Me CN NHCOOEt NSO2NMe2 Me CN NHCOOEt NP(O)(OMe)2 Me CN NHCOOEt NP(O)(OEt)2 Me CN NHCOOEt NP(O)Me2 Me CN NHCOOEt NP(O)Et2 Me CN NHCOOEt NP(O)Me(OMe) Me CN NHCOOEt NP(O)(OPr)2 Me CN NHCOOEt NC(O)C(O)H Me CN NHCOOEt NC(O)C(O)Me Me CN NHCOOEt NC(O)C(O)OMe Me CN NHCOOEt NC(O)C(O)OEt Me CN NHCOOEt NC(O)C(O)NH2 Me CN NHCOOEt NC(O)C(O)OH Me CN NHCOOEt NC(NH)NH2 Me CN NHCOOEt NC(NOH)NH2 Me CN NHCOOEt NC(NH)NHMe Me CN NHCOOEt NC(NH)NMe2 Me CN NHCOOEt NC(NH)OMe Me CN NHCOOEt NC(NH)OEt Et CN NHCOOEt NCOMe Et CN NHCOOEt NCOEt Et CN NHCOOEt NCOPr Et CN NHCOOEt NCHO Et CN NHCOOEt NCOiPr 48

Et CN NHCOOEt NCOtBu Et CN NHCOOEt NCOPh Et CN NHCOOEt NSO2Me Et CN NHCOOEt NSO2Et Et CN NHCOOEt NSO2Pr Et CN NHCOOEt NSO2Ph Et CN NHCOOEt NSO2iPr Et CN NHCOOEt NNO2 Et CN NHCOOEt NCOOMe Et CN NHCOOEt NCOOEt Et CN NHCOOEt NCOOPr Et CN NHCOOEt NCOOiPr Et CN NHCOOEt NCONHEt Et CN NHCOOEt NCONHPr Et CN NHCOOEt NCONH2 Et CN NHCOOEt NCONHMe Et CN NHCOOEt NCN Et CN NHCOOEt NCOSMe Et CN NHCOOEt NCOSEt Et CN NHCOOEt NCSOMe Et CN NHCOOEt NCSOEt Et CN NHCOOEt NCSOPr Et CN NHCOOEt NSO2NH2 Et CN NHCOOEt NSO2NHMe Et CN NHCOOEt NSO2NMe2 Et CN NHCOOEt NP(O)(OMe)2 Et CN NHCOOEt NP(O)(OEt)2 Et CN NHCOOEt NP(O)Me2 49

Et CN NHCOOEt NP(O)Et2 Et CN NHCOOEt NP(O)Me(OMe) Et CN NHCOOEt NP(O)(OPr)2 Et CN NHCOOEt NC(O)C(O)H Et CN NHCOOEt NC(O)C(O)Me Et CN NHCOOEt NC(O)C(O)OMe Et CN NHCOOEt NC(O)C(O)OEt Et CN NHCOOEt NC(O)C(O)NH2 Et CN NHCOOEt NC(O)C(O)OH Et CN NHCOOEt NC(NH)NH2 Et CN NHCOOEt NC(NOH)NH2 Et CN NHCOOEt NC(NH)NHMe Et CN NHCOOEt NC(NH)NMe2 Et CN NHCOOEt NC(NH)OMe Et CN NHCOOEt NC(NH)OEt Me CN NHCH2COOMe NCOMe Me CN NHCH2COOMe NCOEt Me CN NHCH2COOMe NCOPr Me CN NHCH2COOMe NCHO Me CN NHCH2COOMe NCOiPr Me CN NHCH2COOMe NCOtBu Me CN NHCH2COOMe NCOPh Me CN NHCH2COOMe NSO2Me Me CN NHCH2COOMe NSO2Et Me CN NHCH2COOMe NSO2Pr Me CN NHCH2COOMe NSO2Ph Me CN NHCH2COOMe NSO2iPr Me CN NHCH2COOMe NNO2 50

Me CN NHCH2COOMe NCOOMe Me CN NHCH2COOMe NCOOEt Me CN NHCH2COOMe NCOOPr Me CN NHCH2COOMe NCOOiPr Me CN NHCH2COOMe NCONHEt Me CN NHCH2COOMe NCONHPr Me CN NHCH2COOMe NCONH2 Me CN NHCH2COOMe NCONHMe Me CN NHCH2COOMe NCN Me CN NHCH2COOMe NCOSMe Me CN NHCH2COOMe NCOSEt Me CN NHCH2COOMe NCSOMe Me CN NHCH2COOMe NCSOEt Me CN NHCH2COOMe NCSOPr Me CN NHCH2COOMe NSO2NH2 Me CN NHCH2COOMe NSO2NHMe Me CN NHCH2COOMe NSO2NMe2 Me CN NHCH2COOMe NP(O)(OMe)2 Me CN NHCH2COOMe NP(O)(OEt)2 Me CN NHCH2COOMe NP(O)Me2 Me CN NHCH2COOMe NP(O)Et2 Me CN NHCH2COOMe NP(O)Me(OMe) Me CN NHCH2COOMe NP(O)(OPr)2 Me CN NHCH2COOMe NC(O)C(O)H Me CN NHCH2COOMe NC(O)C(O)Me Me CN NHCH2COOMe NC(O)C(O)OMe Me CN NHCH2COOMe NC(O)C(O)OEt Me CN NHCH2COOMe NC(O)C(O)NH2 51

Me CN NHCH2COOMe NC(O)C(O)OH Me CN NHCH2COOMe NC(NH)NH2 Me CN NHCH2COOMe NC(NOH)NH2 Me CN NHCH2COOMe NC(NH)NHMe Me CN NHCH2COOMe NC(NH)NMe2 Me CN NHCH2COOMe NC(NH)OMe Me CN NHCH2COOMe NC(NH)OEt Et CN NHCH2COOMe NCOMe Et CN NHCH2COOMe NCOEt Et CN NHCH2COOMe NCOPr Et CN NHCH2COOMe NCHO Et CN NHCH2COOMe NCOiPr Et CN NHCH2COOMe NCOtBu Et CN NHCH2COOMe NCOPh Et CN NHCH2COOMe NSO2Me Et CN NHCH2COOMe NSO2Et Et CN NHCH2COOMe NSO2Pr Et CN NHCH2COOMe NSO2Ph Et CN NHCH2COOMe NSO2iPr Et CN NHCH2COOMe nno2 Et CN NHCH2COOMe NCOOMe Et CN NHCH2COOMe NCOOEt Et CN NHCH2COOMe NCOOPr Et CN NHCH2COOMe NCOOiPr Et CN NHCH2COOMe NCONHEt Et CN NHCH2COOMe NCONHPr Et CN NHCH2COOMe NCONH2 Et CN NHCH2COOMe NCONHMe 52

Et CN NHCH2COOMe NCN Et CN NHCH2COOMe NCOSMe Et CN NHCH2COOMe NCOSEt Et CN NHCH2COOMe NCSOMe Et CN NHCH2COOMe NCSOEt Et CN NHCH2COOMe NCSOPr Et CN NHCH2COOMe NSO2NH2 Et CN NHCH2COOMe NSO2NHMe Et CN NHCH2COOMe NSO2NMe2 Et CN NHCH2COOMe NP(O)(OMe)2 Et CN NHCH2COOMe NP(O)(OEt)2 Et CN NHCH2COOMe NP(O)Me2 Et CN NHCH2COOMe NP(O)Et2 Et CN NHCH2COOMe NP(O)Me(OMe) Et CN NHCH2COOMe NP(O)(OPr)2 Et CN NHCH2COOMe NC(O)C(O)H Et CN NHCH2COOMe NC(O)C(O)Me Et CN NHCH2COOMe NC(O)C(O)OMe Et CN NHCH2COOMe NC(O)C(O)OEt Et CN NHCH2COOMe NC(O)C(O)NH2 Et CN NHCH2COOMe NC(O)C(O)OH Et CN NHCH2COOMe NC(NH)NH2 Et CN NHCH2COOMe NC(NOH)NH2 Et CN NHCH2COOMe NC(NH)NHMe Et CN NHCH2COOMe NC(NH)NMe2 Et CN NHCH2COOMe NC(NH)OMe Et CN NHCH2COOMe NC(NH)OEt Me CN NHCH2CN NCOMe 53

Me CN NHCH,CN NCOEt Me CN nhch2cn NCOPr Me CN nhch2cn NCHO Me CN nhch2cn NCOiPr Me CN nhch2cn NCOtBu Me CN nhch2cn NCOPh Me CN nhch2cn NSO2Me Me CN nhch2cn NSO2Et Me CN nhch2cn NSO2Pr Me CN nhch2cn NSO2Ph Me CN nhch2cn NSO2iPr Me CN nhch2cn nno2 Me CN nhch2cn NCOOMe Me CN nhch2cn NCOOEt Me CN nhch2cn NCOOPr Me CN nhch2cn NCOOiPr Me CN nhch2cn NCONHEt Me CN nhch2cn NCONHPr Me CN nhch2cn nconh2 Me CN nhch2cn NCONHMe Me CN nhch2cn NCN Me CN nhch2cn NCOSMe Me CN nhch2cn NCOSEt Me CN nhch2cn NCSOMe Me CN nhch2cn NCSOEt Me CN nhch2cn NCSOPr Me CN nhch2cn NSO2NH2 Me CN nhch2cn NSO2NHMe 54

Me CN NHCH2CN NSO2NMe2 Me CN nhch2cn NP(O)(OMe)2 Me CN nhch2cn NP(O)(OEt)2 Me CN nhch2cn NP(O)Me2 Me CN nhch2cn NP(O)Et2 Me CN nhch2cn NP(O)Me(OMe) Me CN nhch2cn NP(O)(OPr)2 Me CN nhch2cn NC(O)C(O)H Me CN nhch2cn NC(O)C(O)Me Me CN nhch2cn NC(O)C(O)OMe Me CN NHCHjCN NC(O)C(O)OEt Me CN nhch2cn NC(O)C(O)NH2 Me CN nhch2cn NC(O)C(O)OH Me CN nhch2cn NC(NH)NH2 Me CN nhch2cn NC(NOH)NH2 Me CN nhch2cn NC(NH)NHMe Me CN nhch2cn NC(NH)NMe2 Me CN nhch2cn NC(NH)OMe Me CN nhch2cn NC(NH)OEt Et CN NHCHaCN NCOMe Et CN nhch2cn NCOEt Et CN nhch2cn NCOPr Et CN nhch2cn NCHO Et CN nhch2cn NCOiPr Et CN nhch2cn NCOtBu Et CN nhch2cn NCOPh Et CN nhch2cn NSO2Me Et CN nhch2cn NSO2Et 55

Et CN NHCH2CN NSOoPr Et CN nhch2cn NSOoPh Et CN nhch2cn NSO2iPr Et CN nhch2cn nno2 Et CN nhch2cn NCOOMe Et CN nhch2cn NCOOEt Et CN nhch2cn NCOOPr Et CN nhch2cn NCOOiPr Et CN nhch2cn NCONHEt Et CN nhch2cn NCONHPr Et CN nhch2cn nconh2 Et CN nhch2cn NCONHMe Et CN nhch2cn NCN Et CN nhch2cn NCOSMe Et CN nhch2cn NCOSEt Et CN nhch2cn NCSOMe Et CN nhch2cn NCSOEt Et CN nhch2cn NCSOPr Et CN nhch2cn NSO2NH2 Et CN nhch2cn NSO2NHMe Et CN nhch2cn NSO2NMe2 Et CN nhch2cn NP(O)(OMe)2 Et CN nhch2cn NP(O)(OEt)2 Et CN nhch2cn NP(O)Me2 Et CN nhch2cn NP(O)Et2 Et CN nhch2cn NP(O)Me(OMe) Et CN nhch2cn NP(O)(OPr)2 Et CN nhch2cn NC(O)C(O)H 56

Et CN NHCH2CN NC(O)C(O)Me Et CN nhch2cn NC(O)C(O)OMe Et CN nhch2cn NC(O)C(O)OEt Et CN nhch2cn NC(O)C(O)NH2 Et CN nhch2cn NC(O)C(O)OH Et CN nhch2cn NC(NH)NH2 Et CN nhch2cn NC(NOH)NH2 Et CN nhch2cn NC(NH)NHMe Et CN nhch2cn NC(NH)NMe2 Et CN nhch2cn NC(NH)OMe Et CN nhch2cn NC(NH)OEt Me CN nhch2conh2 NCOMe Me CN nhch2conh2 NCOEt Me CN nhch2conh2 NCOPr Me CN nhch2conh2 NCHO Me CN nhch2conh2 NCOiPr Me CN nhch2conh2 NCOtBu Me CN nhch2conh2 NCOPh Me CN nhch2conh2 NSO2Me Me CN nhch2conh2 NSO2Et Me CN nhch2conh2 NSO2Pr Me CN nhch2conh2 NSO2Ph Me CN nhch2conh2 NSO2iPr Me CN nhch2conh2 nno2 Me CN nhch2conh2 NCOOMe Me CN nhch2conh2 NCOOEt Me CN nhch2conh2 NCOOPr Me CN nhch2conh2 NCOOiPr 57

Me CN NHCH2CONH2 NCONHEt Me CN nhch2conh2 NCONHPr Me CN nhch2conh2 NCONH2 Me CN nhch2conh2 NCONHMe Me CN nhch2conh2 NCN Me CN nhch2conh2 NCOSMe Me CN nhch2conh2 NCOSEt Me CN nhch2conh2 NCSOMe Me CN nhch2conh2 NCSOEt Me CN nhch2conh2 NCSOPr Me CN nhch2conh2 NSO2NH2 Me CN nhch2conh2 NSO2NHMe Me CN nhch2conh2 NSO2NMe2 Me CN nhch2conh2 NP(O)(OMe)2 Me CN nhch2conh2 NP(O)(OEt)2 Me CN nhch2conh2 NP(O)Me2 Me CN nhch2conh2 NP(O)Et2 Me CN nhch2conh2 NP(O)Me(OMe) Me CN nhch2conh2 NP(O)(OPr)2 Me CN nhch2conh2 NC(O)C(O)H Me CN nhch2conh2 NC(O)C(O)Me Me CN nhch2conh2 NC(O)C(O)OMe Me CN nhch2conh2 NC(O)C(O)OEt Me CN nhch2conh2 NC(O)C(O)NH2 Me CN nhch2conh2 NC(O)C(O)OH Me CN nhch2conh2 NC(NH)NH2 Me CN nhch2conh2 NC(NOH)NH2 Me CN nhch2conh2 NC(NH)NHMe 58

Me CN NHCH2CONH2 NC(NH)NMe2 Me CN nhch2conh2 NC(NH)OMe Me CN nhch2conh2 NC(NH)OEt Et CN nhch2conh2 NCOMe Et CN nhch2conh2 NCOEt Et CN nhch2conh2 NCOPr Et CN nhch2conh2 NCHO Et CN nhch2conh2 NCOiPr Et CN nhch2conh2 NCOtBu Et CN nhch2conh2 NCOPh Et CN nhch2conh2 NSO2Me Et CN nhch2conh2 NSO2Et Et CN nhch2conh2 NSO2Pr Et CN nhch2conh2 NSO2Ph Et CN nhch2conh2 NSO2iPr Et CN nhch2conh2 nno2 Et CN nhch2conh2 NCOOMe Et CN nhch2conh2 NCOOEt Et CN nhch2conh2 NCOOPr Et CN nhch2conh2 NCOOiPr Et CN nhch2conh2 NCONHEt Et CN nhch2conh2 NCONHPr Et CN nhch2conh2 NCONH2 Et CN nhch2conh2 NCONHMe Et CN nhch2conh2 NCN Et CN nhch2conh2 NCOSMe Et CN nhch2conh2 NCOSEt Et CN nhch2conh2 NCSOMe 59

Et CN NHCH2CONH2 NCSOEt Et CN nhch2conh2 NCSOPr Et CN nhch2conh2 NSO2NH2 Et CN nhch2conh2 NSO2NHMe Et CN nhch2conh2 NSO2NMe2 Et CN nhch2conh2 NP(O)(OMe)2 Et CN nhch2conh2 NP(O)(OEt)2 Et CN nhch2conh2 NP(O)Me2 Et CN nhch2conh2 NP(O)Et2 Et CN nhch2conh2 NP(O)Me(OMe) Et CN nhch2conh2 NP(O)(OPr)2 Et CN nhch2conh2 NC(O)C(O)H Et CN nhch2conh2 NC(O)C(O)Me Et CN nhch2conh2 NC(O)C(O)OMe Et CN nhch2conh2 NC(O)C(O)OEt Et CN nhch2conh2 NC(O)C(O)NH2 Et CN nhch2conh2 NC(O)C(O)OH Et CN nhch2conh2 NC(NH)NH2 Et CN nhch2conh2 NC(NOH)NH2 Et CN nhch2conh2 NC(NH)NHMe Et CN nhch2conh2 NC(NH)NMe2 Et CN nhch2conh2 NC(NH)OMe Et CN nhch2conh2 NC(NH)OEt Me CN NHCH2CH2SMe NCOMe Me CN NHCH2CH2SMe NCOEt Me CN NHCH2CH2SMe NCOPr Me CN NHCH2CH2SMe NCHO Me CN NHCH2CH2SMe NCOiPr 60

Me CN NHCH2CH2SMe NCOtBu Me CN NHCH2CH2SMe NCOPh Me CN NHCH2CH2SMe NSO2Me Me CN NHCH2CH2SMe NSO2Et Me CN NHCH2CH2SMe NSO2Pr Me CN NHCH2CH2SMe NSO2Ph Me CN NHCH2CH2SMe NSO2iPr Me CN NHCH2CH2SMe nno2 Me CN NHCH2CH2SMe NCOOMe Me CN NHCH2CH2SMe NCOOEt Me CN NHCH2CH2SMe NCOOPr Me CN NHCH2CH2SMe NCOOiPr Me CN NHCH2CH2SMe NCONHEt Me CN NHCH2CH2SMe NCONHPr Me CN NHCH2CH2SMe NCONH2 Me CN NHCH2CH2SMe NCONHMe Me CN NHCH2CH2SMe NCN Me CN NHCH2CH2SMe NCOSMe Me CN NHCH2CH2SMe NCOSEt Me CN NHCH2CH2SMe NCSOMe Me CN NHCH2CH2SMe NCSOEt Me CN NHCH2CH2SMe NCSOPr Me CN NHCH2CH2SMe NSO2NH2 Me CN NHCH2CH2SMe NSO2NHMe Me CN NHCH2CH2SMe NSO2NMe2 Me CN NHCH2CH2SMe NP(O)(OMe)2 Me CN NHCH2CH2SMe NP(O)(OEt)2 Me CN NHCH2CH2SMe NP(O)Me2 61

Me CN NHCH2CH2SMe NP(O)Et2 Me CN NHCH2CH2SMe NP(O)Me(OMe) Me CN NHCH2CH2SMe NP(O)(OPr)2 Me CN NHCH2CH2SMe NC(O)C(O)H Me CN NHCH2CH2SMe NC(O)C(O)Me Me CN NHCH2CH2SMe NC(O)C(O)OMe Me CN NHCH2CH2SMe NC(O)C(O)OEt Me CN NHCH2CH2SMe NC(O)C(O)NH2 Me CN NHCH2CH2SMe NC(O)C(O)OH Me CN NHCH2CH2SMe NC(NH)NH2 Me CN NHCH2CH2SMe NC(NOH)NH2 Me CN NHCH2CH2SMe NC(NH)NHMe Me CN NHCH2CH2SMe NC(NH)NMe2 Me CN NHCH2CH2SMe NC(NH)OMe Me CN NHCH2CH2SMe NC(NH)OEt Me CN NHCH2CH2SOMe NCOMe Me CN NHCH2CH2SOMe NCOEt Me CN NHCH2CH2SOMe NCOPr Me CN NHCH2CH2SOMe NCHO Me CN NHCH2CH2SOMe NCOiPr Me CN NHCH2CH2SOMe NCOtBu Me CN NHCH2CH2SOMe NCOPh Me CN NHCH2CH2SOMe NSO2Me Me CN NHCH2CH2SOMe NSO2Et Me CN NHCH2CH2SOMe NSO2Pr Me CN NHCH2CH2SOMe NSO2Ph Me CN NHCH2CH2SOMe NS02iPr Me CN NHCH2CH2SOMe nno2 62

Me CN NHCH2CH2SOMe NCOOMe Me CN NHCH2CH2SOMe NCOOEt Me CN NHCH2CH2SOMe NCOOPr Me CN NHCH2CH2SOMe NCOOiPr Me CN NHCH2CH2SOMe NCONHEt Me CN NHCH2CH2SOMe NCONHPr Me CN NHCH2CH2SOMe NCONH2 Me CN NHCH2CH2SOMe NCONHMe Me CN NHCH2CH2SOMe NCN Me CN NHCH2CH2SOMe NCOSMe Me CN NHCH2CH2SOMe NCOSEt Me CN NHCH2CH2SOMe NCSOMe Me CN NHCH2CH2SOMe NCSOEt Me CN NHCH2CH2SOMe NCSOPr Me CN NHCH2CH2SOMe NSO2NH2 Me CN NHCH2CH2SOMe NSO2NHMe Me CN NHCH2CH2SOMe NSO2NMe2 Me CN NHCH2CH2SOMe NP(O)(OMe)2 Me CN NHCH2CH2SOMe NP(O)(OEt)2 Me CN NHCH2CH2SOMe NP(O)Me2 Me CN NHCH2CH2SOMe NP(O)Et2 Me CN NHCH2CH2SOMe NP(O)Me(OMe) Me CN NHCH2CH2SOMe NP(O)(OPr)2 Me CN NHCH2CH2SOMe NC(O)C(O)H Me CN NHCH2CH2SOMe NC(O)C(O)Me Me CN NHCH2CH2SOMe NC(O)C(O)OMe Me CN NHCH2CH2SOMe NC(O)C(O)OEt Me CN NHCH2CH2SOMe NC(O)C(O)NH2 63

Me CN NHCH2CH2SOMe NC(O)C(O)OH Me CN NHCH2CH2SOMe NC(NH)NH2 Me CN NHCH2CH2SOMe NC(NOH)NH2 Me CN NHCH2CH2SOMe NC(NH)NHMe Me CN NHCH2CH2SOMe NC(NH)NMe2 Me CN NHCH2CH2SOMe NC(NH)OMe Me CN NHCH2CH2SOMe NC(NH)OEt Et CN NHCH2CH2SMe NCOMe Et CN NHCH2CH2SMe NCOEt Et CN NHCH2CH2SMe NCOPr Et CN NHCH2CH2SMe NCHO Et CN NHCH2CH2SMe NCOiPr Et CN NHCH2CH2SMe NCOtBu Et CN NHCH2CH2SMe NCOPh Et CN NHCH2CH2SMe NSO2Me Et CN NHCH2CH2SMe NSO2Et Et CN NHCH2CH2SMe NSO2Pr Et CN NHCH2CH2SMe NSO2Ph Et CN NHCH2CH2SMe NSO2iPr Et CN NHCH2CH2SMe nno2 Et CN NHCH2CH2SMe NCOOMe Et CN NHCH2CH2SMe NCOOEt Et CN NHCH2CH2SMe NCOOPr Et CN NHCH2CH2SMe NCOOiPr Et CN NHCH2CH2SMe NCONHEt Et CN NHCH2CH2SMe NCONHPr Et CN NHCH2CH2SMe NCONH2 Et CN NHCH2CH2SMe NCONHMe 64

Et CN NHCH2CH2SMe NCN Et CN NHCH2CH2SMe NCOSMe Et CN NHCH2CH2SMe NCOSEt Et CN NHCH2CH2SMe NCSOMe Et CN NHCH2CH2SMe NCSOEt Et CN NHCH2CH2SMe NCSOPr Et CN NHCH2CH2SMe NSO2NH2 Et CN NHCH2CH2SMe NSO2NHMe Et CN NHCH2CH2SMe NSO2NMe2 Et CN NHCH2CH2SMe NP(O)(OMe)2 Et CN NHCH2CH2SMe NP(O)(OEt)2 Et CN NHCH2CH2SMe NP(O)Me2 Et CN NHCH2CH2SMe NP(O)Et2 Et CN NHCH2CH2SMe NP(O)Me(OMe) Et CN NHCH2CH2SMe NP(O)(OPr)2 Et CN NHCH2CH2SMe NC(O)C(O)H Et CN NHCH2CH2SMe NC(O)C(O)Me Et CN NHCH2CH2SMe NC(O)C(O)OMe Et CN NHCH2CH2SMe NC(O)C(O)OEt Et CN NHCH2CH2SMe NC(O)C(O)NH2 Et CN NHCH2CH2SMe NC(O)C(O)OH Et CN NHCH2CH2SMe NC(NH)NH2 Et CN NHCH2CH2SMe NC(NOH)NH2 Et CN NHCH2CH2SMe NC(NH)NHMe Et CN NHCH2CH2SMe NC(NH)NMe2 Et CN NHCH2CH2SMe NC(NH)OMe Et CN NHCH2CH2SMe NC(NH)OEt Et CN NHCH2CH2SOMe NCOMe 65

Et CN NHCH2CH2SOMe NCOEt Et CN NHCH2CH2SOMe NCOPr Et CN NHCH2CH2SOMe NCHO Et CN NHCH2CH2SOMe NCOiPr Et CN NHCH2CH2SOMe NCOtBu Et CN NHCH2CH2SOMe NCOPh Et CN NHCH2CH2SOMe NSO2Me Et CN NHCH2CH2SOMe NSO2Et Et CN NHCH2CH2SOMe NSO2Pr Et CN NHCH2CH2SOMe NSO2Ph Et CN NHCH2CH2SOMe NSO2iPr Et CN NHCH2CH2SOMe nno2 Et CN NHCH2CH2SOMe NCOOMe Et CN NHCH2CH2SOMe NCOOEt Et CN NHCH2CH2SOMe NCOOPr Et CN NHCH2CH2SOMe NCOOiPr Et CN NHCH2CH2SOMe NCONHEt Et CN NHCH2CH2SOMe NCONHPr Et CN NHCH2CH2SOMe nconh2 Et CN NHCH2CH2SOMe NCONHMe Et CN NHCH2CH2SOMe NCN Et CN NHCH2CH2SOMe NCOSMe Et CN NHCH2CH2SOMe NCOSEt Et CN NHCH2CH2SOMe NCSOMe Et CN NHCH2CH2SOMe NCSOEt Et CN NHCH2CH2SOMe NCSOPr Et CN NHCH2CH2SOMe NSO2NH2 Et CN NHCH2CH2SOMe NSO2NHMe 66

Et CN NHCH2CH2SOMe NSO2NMe2 Et CN NHCH2CH2SOMe NP(O)(OMe)2 Et CN NHCH2CH2SOMe NP(O)(OEt)2 Et CN NHCH2CH2SOMe NP(O)Me2 Et CN NHCH2CH2SOMe NP(O)Et2 Et CN NHCH2CH2SOMe NP(O)Me(OMe) Et CN NHCH2CH2SOMe NP(O)(OPr)2 Et CN NHCH2CH2SOMe NC(O)C(O)H Et CN NHCH2CH2SOMe NC(O)C(O)Me Et CN NHCH2CH2SOMe NC(O)C(O)OMe Et CN NHCH2CH2SOMe NC(O)C(O)OEt Et CN NHCH2CH2SOMe NC(O)C(O)NH2 Et CN NHCH2CH2SOMe NC(O)C(O)OH Et CN NHCH2CH2SOMe NC(NH)NH2 Et CN NHCH2CH2SOMe NC(NOH)NH2 Et CN NHCH2CH2SOMe NC(NH)NHMe Et CN NHCH2CH2SOMe NC(NH)NMe2 Et CN NHCH2CH2SOMe NC(NH)OMe Et CN NHCH2CH2SOMe NC(NH)OEt Me CN NHCOMe NCOMe 0 Me CN NHCOMe NCOEt 0 Me CN NHCOMe NCOPr 0 Me CN NHCOMe NCHO 0 Me CN NHCOMe NCOiPr 0 Me CN NHCOMe NCOtBu 0 Me CN NHCOMe NCOPh 0 Me CN NHCOMe NSO2Me 0 Me CN NHCOMe NSO2Et 0 67

Me CN NHCOMe NSO2Pr 0 Me CN NHCOMe NSO2Ph 0 Me CN NHCOMe NSO2iPr 0 Me CN NHCOMe nno2 0 Me CN NHCOMe NCOOMe 0 Me CN NHCOMe NCOOEt 0 Me CN NHCOMe NCOOPr 0 Me CN NHCOMe NCOOiPr 0 Me CN NHCOMe NCONHEt 0 Me CN NHCOMe NCONHPr 0 Me CN NHCOMe nconh2 0 Me CN NHCOMe NCONHMe 0 Me CN NHCOMe NCN 0 Me CN NHCOMe NCOSMe 0 Me CN NHCOMe NCOSEt 0 Me CN NHCOMe NCSOMe 0 Me CN NHCOMe NCSOEt 0 Me CN NHCOMe NCSOPr 0 Me CN NHCOMe nso2nh2 0 Me CN NHCOMe NSO2NHMe 0 Me CN NHCOMe NSO2NMe2 0 Me CN NHCOMe NP(O)(OMe)2 0 Me CN NHCOMe NP(O)(OEt)2 0 Me CN NHCOMe NP(O)Me2 0 Me CN NHCOMe NP(O)Et2 0 Me CN NHCOMe NP(O)Me(OMe) 0 Me CN NHCOMe NP(O)(OPr)2 0 Me CN NHCOMe NC(O)C(O)H 0 68

Me CN NHCOMe NC(O)C(O)Me 0 Me CN NHCOMe NC(O)C(O)OMe 0 Me CN NHCOMe NC(O)C(O)OEt 0 Me CN NHCOMe NC(O)C(O)NH2 0 Me CN NHCOMe NC(O)C(O)OH 0 Me CN NHCOMe NC(NH)NH2 0 Me CN NHCOMe NC(NOH)NH2 0 Me CN NHCOMe NC(NH)NHMe 0 Me CN NHCOMe NC(NH)NMe2 0 Me CN NHCOMe NC(NH)OMe 0 Me CN NHCOMe NC(NH)OEt 0 Et CN NHCOMe NCOMe 0 Et CN NHCOMe NCOEt 0 Et CN NHCOMe NCOPr 0 Et CN NHCOMe NCHO 0 Et CN NHCOMe NCOiPr 0 Et CN NHCOMe NCOtBu 0 Et CN NHCOMe NCOPh O Et CN NHCOMe NSO2Me 0 Et CN NHCOMe NSO2Et 0 Et CN NHCOMe NSO2Pr 0 Et CN NHCOMe NSO2Ph 0 Et CN NHCOMe NSO2iPr 0 Et CN NHCOMe NNO2 0 Et CN NHCOMe NCOOMe 0 Et CN NHCOMe NCOOEt 0 Et CN NHCOMe NCOOPr 0 Et CN NHCOMe NCOOiPr 0 69

Et CN NHCOMe NCONHEt 0 Et CN NHCOMe NCONHPr 0 Et CN NHCOMe nconh2 0 Et CN NHCOMe NCONHMe 0 Et CN NHCOMe NCN 0 Et CN NHCOMe NCOSMe 0 Et CN NHCOMe NCOSEt o Et CN NHCOMe NCSOMe o Et CN NHCOMe NCSOEt 0 Et CN NHCOMe NCSOPr 0 Et CN NHCOMe NSO2NH2 0 Et CN NHCOMe NSO2NHMe 0 Et CN NHCOMe NSO2NMe2 0 Et CN NHCOMe NP(O)(OMe)2 0 Et CN NHCOMe NP(O)(OEt)2 0 Et CN NHCOMe NP(O)Me2 0 Et CN NHCOMe NP(O)Et2 o Et CN NHCOMe NP(O)Me(OMe) 0 Et CN NHCOMe NP(O)(OPr)2 0 Et CN NHCOMe NC(O)C(O)H 0 Et CN NHCOMe NC(O)C(O)Me 0 Et CN NHCOMe NC(O)C(O)OMe 0 Et CN NHCOMe NC(O)C(O)OEt 0 Et CN NHCOMe NC(O)C(O)NH2 0 Et CN NHCOMe NC(O)C(O)OH 0 Et CN NHCOMe NC(NH)NH2 0 Et CN NHCOMe NC(NOH)NH2 0 Et CN NHCOMe NC(NH)NHMe 0 70

Et CN NHCOMe NC(NH)NMe2 0 Et CN NHCOMe NC(NH)OMe 0 Et CN NHCOMe NC(NH)OEt 0 Me CN NHCOOMe NCOMe 0 Me CN NHCOOMe NCOEt 0 Me CN NHCOOMe NCOPr 0 Me CN NHCOOMe NCHO 0 Me CN NHCOOMe NCOiPr 0 Me CN NHCOOMe NCOtBu 0 Me CN NHCOOMe NCOPh 0 Me CN NHCOOMe NSO2Me 0 Me CN NHCOOMe NSO2Et 0 Me CN NHCOOMe NSO2Pr 0 Me CN NHCOOMe NSO2Ph 0 Me CN NHCOOMe NSO2iPr 0 Me CN NHCOOMe nno2 0 Me CN NHCOOMe NCOOMe 0 Me CN NHCOOMe NCOOEt 0 Me CN NHCOOMe NCOOPr 0 Me CN NHCOOMe NCOOiPr 0 Me CN NHCOOMe NCONHEt 0 Me CN NHCOOMe NCONHPr 0 Me CN NHCOOMe nconh2 0 Me CN NHCOOMe NCONHMe 0 Me CN NHCOOMe NCN 0 Me CN NHCOOMe NCOSMe 0 Me CN NHCOOMe NCOSEt 0 Me CN NHCOOMe NCSOMe 0 71

Me CN NHCOOMe NCSOEt 0 Me CN NHCOOMe NCSOPr 0 Me CN NHCOOMe NSO2NH2 0 Me CN NHCOOMe NSO2NHMe 0 Me CN NHCOOMe NSO2NMe2 0 Me CN NHCOOMe NP(O)(OMe)2 0 Me CN NHCOOMe NP(0)(0Et)2 0 Me CN NHCOOMe NP(O)Me2 0 Me CN NHCOOMe NP(O)Et2 0 Me CN NHCOOMe NP(O)Me(OMe) 0 Me CN NHCOOMe NP(O)(OPr)2 0 Me CN NHCOOMe NC(O)C(O)H 0 Me CN NHCOOMe NC(O)C(O)Me O Me CN NHCOOMe NC(O)C(O)OMe 0 Me CN NHCOOMe NC(O)C(O)OEt 0 Me CN NHCOOMe NC(O)C(O)NH2 0 Me CN NHCOOMe NC(O)C(O)OH 0 Me CN NHCOOMe NC(NH)NH2 0 Me CN NHCOOMe NC(NOH)NH2 0 Me CN NHCOOMe NC(NH)NHMe 0 Me CN NHCOOMe NC(NH)NMe2 0 Me CN NHCOOMe NC(NH)OMe 0 Me CN NHCOOMe NC(NH)OEt 0 Et CN NHCOOMe NCOMe 0 Et CN NHCOOMe NCOEt 0 Et CN NHCOOMe NCOPr 0 Et CN NHCOOMe NCHO 0 Et CN NHCOOMe NCOiPr 0 72

Et CN NHCOOMe NCOtBu Et CN NHCOOMe NCOPh Et CN NHCOOMe NSO2Me Et CN NHCOOMe NSO2Et Et CN NHCOOMe NSO2Pr Et CN NHCOOMe NSO2Ph Et CN NHCOOMe NSO2iPr Et CN NHCOOMe NNO2 Et CN NHCOOMe NCOOMe Et CN NHCOOMe NCOOEt Et CN NHCOOMe NCOOPr Et CN NHCOOMe NCOOiPr Et CN NHCOOMe NCONHEt Et CN NHCOOMe NCONHPr Et CN NHCOOMe nconh2 Et CN NHCOOMe NCONHMe Et CN NHCOOMe NCN Et CN NHCOOMe NCOSMe Et CN NHCOOMe NCOSEt Et CN NHCOOMe NCSOMe Et CN NHCOOMe NCSOEt Et CN NHCOOMe NCSOPr Et CN NHCOOMe NSO2NH2 Et CN NHCOOMe NSO2NHMe Et CN NHCOOMe NSO2NMe2 Et CN NHCOOMe NP(O)(OMe)2 Et CN NHCOOMe NP(O)(OEt)2 Et CN NHCOOMe NP(O)Me2 Ο Ο Ο Ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο

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73

Et CN NHCOOMe NP(O)Et2 0 Et CN NHCOOMe NP(O)Me(OMe) 0 Et CN NHCOOMe NP(O)(OPr)2 0 Et CN NHCOOMe NC(O)C(O)H 0 Et CN NHCOOMe NC(O)C(O)Me 0 Et CN NHCOOMe NC(O)C(O)OMe 0 Et CN NHCOOMe NC(O)C(O)OEt 0 Et CN NHCOOMe NC(O)C(O)NH2 0 Et CN NHCOOMe NC(O)C(O)OH 0 Et CN NHCOOMe NC(NH)NH2 0 Et CN NHCOOMe NC(NOH)NH2 0 Et CN NHCOOMe NC(NH)NHMe 0 Et CN NHCOOMe NC(NH)NMe2 0 Et CN NHCOOMe NC(NH)OMe 0 Et CN NHCOOMe NC(NH)OEt o cf3 CN nh2 NCOMe cf3 CN nh2 NCOEt cf3 CN nh2 NCOPr cf3 CN nh2 NCHO cf3 CN nh2 NCOiPr cf3 CN nh2 NCOtBu cf3 CN nh2 NCOPh cf3 CN nh2 NSO2Me cf3 CN nh2 NSO2Et cf3 CN nh2 NSO2Pr cf3 CN nh2 NSO2Ph cf3 CN nh2 NSO2iPr cf3 CN nh2 NNO2 74 cf3 CN nh2 NCOOMe cf3 CN nh2 NCOOEt cf3 CN nh2 NCOOPr cf3 CN nh2 NCOOiPr cf3 CN nh2 NCONHEt cf3 CN nh2 NCONHPr cf3 CN nh2 NCONH2 cf3 CN nh2 NCONHMe cf3 CN nh2 NCN cf3 CN nh2 NCOSMe cf3 CN nh2 NCOSEt cf3 CN nh2 NCSOMe cf3 CN nh2 NCSOEt cf3 CN nh2 NCSOPr cf3 CN nh2 NSO2NH2 cf3 CN nh2 NSO2NHMe cf3 CN nh2 NSO2NMe2 cf3 CN nh2 NP(O)(OMe)2 cf3 CN nh2 NP(O)(OEt)2 cf3 CN nh2 NP(O)Me2 cf3 CN nh2 NP(O)Et2 cf3 CN nh2 NP(O)Me(OMe) cf3 CN nh2 NP(O)(OPr)2 cf3 CN nh2 NC(O)C(O)H cf3 CN nh2 NC(O)C(O)Me cf3 CN nh2 NC(O)C(O)OMe cf3 CN nh2 NC(O)C(O)OEt cf3 CN nh2 NC(O)C(O)NH2 75 cf3 CN NH2 NC(O)C(O)OH cf3 CN nh2 NC(NH)NH2 cf3 CN nh2 NC(NOH)NH2 cf3 CN nh2 NC(NH)NHMe cf3 CN nh2 NC(NH)NMe2 cf3 CN nh2 NC(NH)OMe cf3 CN nh2 NC(NH)OEt cf3 CN NHMe NCOMe cf3 CN NHMe NCOEt cf3 CN NHMe NCOPr cf3 CN NHMe NCHO cf3 CN NHMe NCOiPr cf3 CN NHMe NCOtBu cf3 CN NHMe NCOPh cf3 CN NHMe NSO2Me cf3 CN NHMe NSO2Et cf3 CN NHMe NSO2Pr cf3 CN NHMe NSO2Ph cf3 CN NHMe NSO2iPr cf3 CN NHMe NNO2 cf3 CN NHMe NCOOMe cf3 CN NHMe NCOOEt cf3 CN NHMe NCOOPr cf3 CN NHMe NCOOiPr cf3 CN NHMe NCONHEt cf3 CN NHMe NCONHPr cf3 CN NHMe NCONH2 cf3 CN NHMe NCONHMe 76 cf3 CN NHMe NCN cf3 CN NHMe NCOSMe cf3 CN NHMe NCOSEt cf3 CN NHMe NCSOMe cf3 CN NHMe NCSOEt cf3 CN NHMe NCSOPr cf3 CN NHMe NSO2NH2 cf3 CN NHMe NSO2NHMe cf3 CN NHMe NSO2NMe2 cf3 CN NHMe NP(O)(OMe)2 cf3 CN NHMe NP(O)(OEt)2 cf3 CN NHMe NP(O)Me2 cf3 CN NHMe NP(O)Et2 cf3 CN NHMe NP(O)Me(OMe) cf3 CN NHMe NP(O)(OPr)2 cf3 CN NHMe NC(O)C(O)H cf3 CN NHMe NC(O)C(O)Me cf3 CN NHMe NC(O)C(O)OMe cf3 CN NHMe NC(O)C(O)OEt cf3 CN NHMe NC(O)C(O)NH2 cf3 CN NHMe NC(O)C(O)OH cf3 CN NHMe NC(NH)NH2 cf3 CN NHMe NC(NOH)NH2 cf3 CN NHMe NC(NH)NHMe cf3 CN NHMe NC(NH)NMe2 cf3 CN NHMe NC(NH)OMe cf3 CN NHMe NC(NH)OEt cf3 CN NHEt NCOMe 77 cf3 CN NHEt NCOEt cf3 CN NHEt NCOPr cf3 CN NHEt NCHO cf3 CN NHEt NCOiPr cf3 CN NHEt NCOtBu cf3 CN NHEt NCOPh cf3 CN NHEt NSO2Me cf3 CN NHEt NSO2Et cf3 CN NHEt NSO2Pr cf3 CN NHEt NSO2Ph cf3 CN NHEt NSO2iPr cf3 CN NHEt NNO2 cf3 CN NHEt NCOOMe cf3 CN NHEt NCOOEt cf3 CN NHEt NCOOPr cf3 CN NHEt NCOOiPr cf3 CN NHEt NCONHEt cf3 CN NHEt NCONHPr cf3 CN NHEt NCONH2 cf3 CN NHEt NCONHMe cf3 CN NHEt NCN cf3 CN NHEt NCOSMe cf3 CN NHEt NCOSEt cf3 CN NHEt NCSOMe cf3 CN NHEt NCSOEt cf3 CN NHEt NCSOPr cf3 CN NHEt NSO2NH2 cf3 CN NHEt NSO2NHMe 78 CF3 CN NHEt NSO2NMe2 cf3 CN NHEt NP(O)(OMe)2 cf3 CN NHEt NP(O)(OEt)2 cf3 CN NHEt NP(O)Me2 cf3 CN NHEt NP(O)Et2 cf3 CN NHEt NP(O)Me(OMe) cf3 CN NHEt NP(O)(OPr)2 cf3 CN NHEt NC(O)C(O)H cf3 . CN NHEt NC(O)C(O)Me cf3 CN NHEt NC(O)C(O)OMe cf3 CN NHEt NC(O)C(O)OEt cf3 CN NHEt NC(O)C(O)NH2 cf3 CN NHEt NC(O)C(O)OH cf3 CN NHEt NC(NH)NH2 cf3 CN NHEt NC(NOH)NH2 cf3 CN NHEt NC(NH)NHMe cf3 CN NHEt NC(NH)NMe2 cf3 CN NHEt NC(NH)OMe cf3 CN NHEt NC(NH)OEt cf3 CN NHCOMe NCOMe cf3 CN NHCOMe NCOEt cf3 CN NHCOMe NCOPr cf3 CN NHCOMe NCHO cf3 CN NHCOMe NCOiPr cf3 CN NHCOMe NCOtBu cf3 CN NHCOMe NCOPh cf3 CN NHCOMe NSO2Me cf3 CN NHCOMe NSO2Et 79

cf3 CN NHCOMe NSO2Pr cf3 CN NHCOMe NSO2Ph cf3 CN NHCOMe NSO2iPr cf3 CN NHCOMe nno2 cf3 CN NHCOMe NCOOMe cf3 CN NHCOMe NCOOEt cf3 CN NHCOMe NCOOPr cf3 CN NHCOMe NCOOiPr cf3 CN NHCOMe NCONHEt cf3 CN NHCOMe NCONHPr cf3 CN NHCOMe NCONH2 cf3 CN NHCOMe NCONHMe cf3 CN NHCOMe NCN cf3 CN NHCOMe NCOSMe cf3 CN NHCOMe NCOSEt cf3 CN NHCOMe NCSOMe cf3 CN NHCOMe NCSOEt cf3 CN NHCOMe NCSOPr cf3 CN NHCOMe NSO2NH2 cf3 CN NHCOMe NSO2NHMe cf3 CN NHCOMe NSO2NMe2 cf3 CN NHCOMe NP(O)(OMe)2 cf3 CN NHCOMe NP(O)(OEt)2 cf3 CN NHCOMe NP(O)Me2 cf3 CN NHCOMe NP(O)Et2 cf3 CN NHCOMe NP(O)Me(OMe) cf3 CN NHCOMe NP(O)(OPr)2 cf3 CN NHCOMe NC(O)C(O)H 80 cf3 CN NHCOMe NC(O)C(O)Me cf3 CN NHCOMe NC(O)C(O)OMe cf3 CN NHCOMe NC(O)C(O)OEt cf3 CN NHCOMe NC(O)C(O)NH2 cf3 CN NHCOMe NC(O)C(O)OH cf3 CN NHCOMe NC(NH)NH2 cf3 CN NHCOMe NC(NOH)NH2 cf3 CN NHCOMe NC(NH)NHMe cf3 CN NHCOMe NC(NH)NMe2 cf3 CN NHCOMe NC(NH)OMe cf3 CN NHCOMe NC(NH)OEt cf3 CN nh2 NCOMe 0 cf3 CN nh2 NH 0 cf3 CN nh2 NCOEt 0 cf3 CN nh2 NCOPr 0 cf3 CN nh2 NCHO 0 cf3 CN nh2 NCOiPr 0 cf3 CN nh2 NCOtBu 0 cf3 CN nh2 NCOPh 0 cf3 CN nh2 NSO2Me 0 cf3 CN nh2 NSO2Et 0 cf3 CN nh2 NSO2Pr 0 cf3 CN nh2 NSO2Ph 0 cf3 CN nh2 NSO2iPr 0 cf3 CN nh2 nno2 0 cf3 CN nh2 NCOOMe 0 cf3 CN nh2 NCOOEt 0 cf3 CN nh2 NCOOPr 0 81 cf3 CN NH, NCOOiPr 0 cf3 CN nh2 NCONHEt 0 cf3 CN. nh2 NCONHPr 0 cf3 CN nh2 NCONH2 0 cf3 CN nh2 NCONHMe 0 cf3 CN nh2 NCN 0 cf3 CN nh2 NCOSMe 0 cf3 CN nh2 NCOSEt 0 cf3 CN nh2 NCSOMe 0 cf3 CN nh2 NCSOEt 0 cf3 CN nh2 NCSOPr 0 cf3 CN nh2 NSO2NH2 0 cf3 CN nh2 NSO2NHMe 0 cf3 CN nh2 NSO2NMe2 0 cf3 CN nh2 NP(O)(OMe)2 0 cf3 CN nh2 NP(O)(OEt)2 0 cf3 CN nh2 NP(O)Me2 0 cf3 CN nh2 NP(O)Et2 0 cf3 CN nh2 NP(O)Me(OMe) 0 cf3 CN nh2 NP(O)(OPr)2 0 cf3 CN nh2 NC(O)C(O)H 0 cf3 CN nh2 NC(O)C(O)Me 0 cf3 CN nh2 NC(O)C(O)OMe 0 cf3 CN nh2 NC(O)C(O)OEt 0 cf3 CN nh2 NC(O)C(O)NH2 0 cf3 CN nh2 NC(O)C(O)OH 0 cf3 CN nh2 NC(NH)NH2 0 cf3 CN nh2 NC(NOH)NH2 0 82 cf3 CN NH2 NC(NH)NHMe 0 cf3 CN nh2 NC(NH)NMe2 0 cf3 CN nh2 NC(NH)OMe 0 cf3 CN nh2 NC(NH)OEt 0 cf3 CN NHMe NCOMe 0 cf3 CN NHMe NCOEt O cf3 CN NHMe NCOPr 0 cf3 CN NHMe NCHO 0 cf3 CN NHMe NCOiPr O cf3 CN NHMe NCOtBu O cf3 CN NHMe NCOPh 0 cf3 CN NHMe NSO2Me 0 cf3 CN NHMe NSO2Et 0 cf3 CN NHMe NSO2Pr 0 cf3 CN NHMe NSO2Ph 0 cf3 CN NHMe NSO2iPr 0 cf3 CN NHMe NNO2 0 cf3 CN NHMe NCOOMe 0 cf3 CN NHMe NCOOEt 0 cf3 CN NHMe NCOOPr 0 cf3 CN NHMe NCOOiPr 0 cf3 CN NHMe NCONHEt 0 cf3 CN NHMe NCONHPr 0 cf3 CN NHMe nconh2 0 cf3 CN NHMe NCONHMe 0 cf3 CN NHMe NCN 0 cf3 CN NHMe NCOSMe 0 cf3 CN NHMe NCOSEt 0 83 cf3 CN NHMe NCSOMe 0 cf3 CN NHMe NCSOEt 0 cf3 CN NHMe NCSOPr 0 cf3 CN NHMe NSO2NH2 O cf3 CN NHMe NSO2NHMe 0 cf3 CN NHMe NSO2NMe2 0 cf3 CN NHMe NP(O)(OMe)2 0 cf3 CN NHMe NP(O)(OEt)2 0 cf3 CN NHMe NP(O)Me2 0 cf3 CN NHMe NP(O)Et2 0 cf3 CN NHMe NP(O)Me(OMe) 0 cf3 CN NHMe NP(O)(OPr)2 0 cf3 CN NHMe NC(O)C(O)H 0 cf3 CN NHMe NC(O)C(O)Me 0 cf3 CN NHMe NC(O)C(O)OMe 0 cf3 CN NHMe NC(O)C(O)OEt 0 cf3 CN NHMe NC(O)C(O)NH2 0 cf3 CN NHMe NC(O)C(O)OH 0 cf3 CN NHMe NC(NH)NH2 0 cf3 CN NHMe NC(NOH)NH2 O cf3 CN NHMe NC(NH)NHMe 0 cf3 CN NHMe NC(NH)NMe2 0 cf3 CN NHMe NC(NH)OMe 0 cf3 CN NHMe NC(NH)OEt 0 cf3 CN NHEt NCOMe 0 cf3 CN NHEt NCOEt 0 cf3 CN NHEt NCOPr 0 cf3 CN NHEt NCHO 0 84 cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt cf3 CN NHEt NCOiPr Ο NCOtBu Ο NCOPh Ο NSO2Me Ο NSO2Et Ο NSO2Pr Ο NSO2Ph Ο NSO2iPr Ο NNO2 Ο NCOOMe Ο NCOOEt Ο NCOOPr Ο NCOOiPr Ο NCONHEt Ο NCONHPr Ο NCONH2 Ο NCONHMe Ο NCN Ο NCOSMe Ο NCOSEt Ο NCSOMe Ο NCSOEt Ο NCSOPr Ο NSO2NH2 Ο NSO2NHMe Ο NSO2NMe2 Ο NP(O)(OMe)2 Ο NP(O)(OEt)2 Ο 85 cf3 CN NHEt NP(O)Me? 0 cf3 CN NHEt NP(O)Et2 0 cf3 CN NHEt NP(O)Me(OMe) 0 cf3 CN NHEt NP(O)(OPr)2 0 cf3 CN NHEt NC(O)C(O)H 0 cf3 CN NHEt NC(O)C(O)Me 0 cf3 CN NHEt NC(O)C(O)OMe 0 cf3 CN NHEt NC(O)C(O)OEt O cf3 CN NHEt NC(O)C(O)NH2 0 cf3 CN NHEt NC(O)C(O)OH 0 cf3 CN NHEt NC(NH)NH2 0 cf3 CN NHEt NC(NOH)NH2 0 cf3 CN NHEt NC(NH)NHMe 0 cf3 CN NHEt NC(NH)NMe2 0 cf3 CN NHEt NC(NH)OMe 0 cf3 CN NHEt NC(NH)OEt 0 cci2f CN nh2 NCOMe cci2f CN nh2 NCOEt cci2f CN nh2 NCOPr cci2f CN nh2 NCHO cci2f CN nh2 NCOiPr cci2f CN nh2 NCOtBu cci2f CN nh2 NCOPh cci2f CN nh2 NSO2Me cci2f CN nh2 NSO2Et cci2f CN nh2 NSO2Pr cci2f CN nh2 NSO2Ph cci2f CN nh2 NSO2iPr 86 cci2f CN nh2 nno2 cci2f CN nh2 NCOOMe cci2f CN nh2 NCOOEt cci2f CN nh2 NCOOPr cci2f CN nh2 NCOOiPr cci2f CN nh2 NCONHEt cci2f CN nh2 NCONHPr cci2f CN nh2 nconh2 cci2f CN nh2 NCONHMe cci2f CN nh2 NCN cci2f CN nh2 NCOSMe cci2f CN nh2 NCOSEt cci2f CN nh2 NCSOMe cci2f CN nh2 NCSOEt cci2f CN nh2 NCSOPr cci2f CN nh2 NSO2NH2 cci2f CN nh2 NSO2NHMe cci2f . CN nh2 NSO2NMe2 cci2f CN nh2 NP(O)(OMe)2 cci2f CN nh2 NP(O)(OEt)2 cci2f CN nh2 NP(O)Me2 cci2f CN nh2 NP(O)Et2 cci2f CN nh2 NP(O)Me(OMe) cci2f CN nh2 NP(O)(OPr)2 cci2f CN nh2 NC(O)C(O)H cci2f CN nh2 NC(O)C(O)Me cci2f CN nh2 NC(O)C(O)OMe cci2f CN nh2 NC(O)C(O)OEt 87 CC12F CN NH2 NC(O)C(O)NH2 cci2f CN nh2 NC(O)C(O)OH cci2f CN nh2 NC(NH)NH2 cci2f CN nh2 NC(NOH)NH2 cci2f CN nh2 NC(NH)NHMe cci2f CN nh2 NC(NH)NMe2 cci2f CN nh2 NC(NH)OMe cci2f CN nh2 NC(NH)OEt cci2f CN NHMe NCOMe cci2f CN NHMe NCOEt cci2f CN NHMe NCOPr cci2f CN NHMe NCHO cci2f CN NHMe NCOiPr cci2f CN NHMe NCOtBu cci2f CN NHMe NCOPh cci2f CN NHMe NSO2Me cci2f CN NHMe NSO2Et cci2f CN NHMe NSO2Pr cci2f CN NHMe NSO2Ph cci2f CN NHMe NSO2iPr cci2f CN NHMe NNO2 cci2f CN NHMe NCOOMe cci2f CN NHMe NCOOEt cci2f CN NHMe NCOOPr cci2f CN NHMe NCOOiPr cci2f CN NHMe NCONHEt cci2f CN NHMe NCONHPr cci2f CN NHMe NCONH2 88 CC12F CN NHMe NCONHMe cci2f CN NHMe NCN cci2f CN NHMe NCOSMe cci2f CN NHMe NCOSEt cci2f CN NHMe NCSOMe cci2f CN NHMe NCSOEt cci2f CN NHMe NCSOPr cci2f CN NHMe nso2nh2 cci2f CN NHMe NSO2NHMe cci2f CN NHMe NSO2NMe2 cci2f CN NHMe NP(O)(OMe)2 cci2f CN NHMe NP(O)(OEt)2 cci2f CN NHMe NP(O)Me2 cci2f CN NHMe NP(O)Et2 cci2f CN NHMe NP(O)Me(OMe) cci2f CN NHMe NP(O)(OPr)2 cci2f CN NHMe NC(O)C(O)H cci2f CN NHMe NC(O)C(O)Me cci2f CN NHMe NC(O)C(O)OMe cci2f CN NHMe NC(O)C(O)OEt cci2f CN NHMe NC(O)C(O)NH2 cci2f CN NHMe NC(O)C(O)OH cci2f CN NHMe NC(NH)NH2 cci2f CN NHMe NC(NOH)NH2 cci2f CN NHMe NC(NH)NHMe cci2f CN NHMe NC(NH)NMe2 cci2f CN NHMe NC(NH)OMe cci2f CN NHMe NC(NH)OEt 89 CC12F CN NHEt NCOMe CC12F CN NHEt NCOEt cci2f CN NHEt NCOPr cci2f CN NHEt NCHO cci2f CN NHEt NCOiPr cci2f CN NHEt NCOtBu cci2f CN NHEt NCOPh cci2f CN NHEt NSO2Me cci2f CN NHEt NSO2Et cci2f CN NHEt NSO2Pr cci2f CN NHEt NSO2Ph cci2f CN NHEt NSO2iPr cci2f CN NHEt nno2 cci2f CN NHEt NCOOMe cci2f CN NHEt NCOOEt cci2f CN NHEt NCOOPr cci2f CN NHEt NCOOiPr cci2f CN NHEt NCONHEt cci2f CN NHEt NCONHPr cci2f CN NHEt nconh2 cci2f CN NHEt NCONHMe cci2f CN NHEt NCN cci2f CN NHEt NCOSMe cci2f CN NHEt NCOSEt cci2f CN NHEt NCSOMe cci2f CN NHEt NCSOEt cci2f CN NHEt NCSOPr cci2f CN NHEt NSO2NH2 90 CC1,F CN NHEt NSO2NHMe CC12F CN NHEt NSO2NMe2 cci2f CN NHEt NP(O)(OMe)2 cci2f CN NHEt NP(0)(0Et)2 cci2f CN NHEt NP(O)Me2 cci2f CN NHEt NP(O)Et2 cci2f CN NHEt NP(O)Me(OMe) cci2f CN NHEt NP(O)(OPr)2 cci2f CN NHEt NC(O)C(O)H cci2f CN NHEt NC(O)C(O)Me cci2f CN NHEt NC(O)C(O)OMe cci2f CN NHEt NC(O)C(O)OEt cci2f CN NHEt NC(O)C(O)NH2 cci2f CN NHEt NC(O)C(O)OH cci2f CN NHEt NC(NH)NH2 cci2f CN NHEt NC(NOH)NH2 cci2f CN NHEt NC(NH)NHMe cci2f CN NHEt NC(NH)NMe2 cci2f CN NHEt NC(NH)OMe cci2f CN NHEt NC(NH)OEt cci2f CN NH2 NH 0 cci2f CN nh2 NCOMe 0 cci2f CN nh2 NCOEt 0 cci2f CN nh2 NCOPr 0 cci2f CN nh2 NCHO 0 cci2f CN nh2 NCOiPr 0 cci2f CN nh2 NCOtBu 0 cci2f CN nh2 NCOPh 0 91 CC12F CN nh2 NSOoMe 0 cci2f CN nh2 NSO2Et 0 cci2f CN nh2 NSO2Pr 0 cci2f CN nh2 NSO2Ph 0 cci2f CN nh2 NSO2iPr 0 cci2f CN nh2 nno2 0 cci2f CN nh2 NCOOMe O cci2f CN nh2 NCOOEt 0 cci2f CN nh2 NCOOPr 0 cci2f CN nh2 NCOOiPr 0 cci2f CN nh2 NCONHEt 0 cci2f CN nh2 NCONHPr 0 cci2f CN nh2 NCONH2 0 cci2f CN nh2 NCONHMe 0 cci2f CN nh2 NCN 0 cci2f CN nh2 NCOSMe O cci2f CN nh2 NCOSEt 0 cci2f CN nh2 NCSOMe 0 cci2f CN nh2 NCSOEt 0 cci2f CN nh2 NCSOPr 0 cci2f CN nh2 NSO2NH2 0 cci2f CN nh2 NSO2NHMe O cci2f CN nh2 NSO2NMe2 0 cci2f CN nh2 NP(O)(OMe)2 0 cci2f CN nh2 NP(O)(OEt)2 0 cci2f CN nh2 NP(O)Me2 0 cci2f CN nh2 NP(O)Et2 0 cci2f CN nh2 NP(O)Me(OMe) 0 92 CCUF CN nh2 NP(O)(OPr)2 0 CC12F CN nh2 NC(O)C(O)H 0 cci2f CN nh2 NC(O)C(O)Me 0 cci2f CN nh2 NC(O)C(O)OMe 0 cci2f CN nh2 NC(O)C(O)OEt O cci2f CN nh2 NC(O)C(O)NH2 0 cci2f CN nh2 NC(O)C(O)OH 0 cci2f CN nh2 NC(NH)NH2 O cci2f CN nh2 NC(NOH)NH2 0 cci2f CN nh2 NC(NH)NHMe 0 cci2f CN nh2 NC(NH)NMe2 0 cci2f CN nh2 NC(NH)OMe 0 cci2f CN nh2 NC(NH)OEt 0 cci2f CN NHMe NCOMe 0 cci2f CN NHMe NCOEt 0 cci2f CN NHMe NCOPr 0 cci2f CN NHMe NCHO 0 cci2f CN NHMe NCOiPr 0 cci2f CN NHMe NCOtBu 0 cci2f CN NHMe NCOPh 0 cci2f CN NHMe NSO2Me 0 cci2f CN NHMe NSO2Et 0 cci2f CN NHMe NSO2Pr 0 cci2f CN NHMe NSO2Ph 0 cci2f CN NHMe NSO2iPr 0 cci2f CN NHMe nno2 0 cci2f CN NHMe NCOOMe 0 cci2f CN NHMe NCOOEt 0

I CC12F CN NHMe NCOOPr 0 cci2f CN NHMe NCOOiPr 0 cci2f CN NHMe NCONHEt o cci2f CN NHMe NCONHPr 0 cci2f CN NHMe NCONH2 0 cci2f CN NHMe NCONHMe 0 cci2f CN NHMe NCN 0 cci2f CN NHMe NCOSMe 0 cci2f CN NHMe NCOSEt 0 cci2f CN NHMe NCSOMe 0 cci2f CN NHMe NCSOEt 0 cci2f CN NHMe NCSOPr o cci2f CN NHMe NSO2NH2 0 cci2f CN NHMe NSO2NHMe 0 cci2f CN NHMe NSO2NMe2 0 cci2f CN NHMe NP(O)(OMe)2 0 cci2f CN NHMe NP(O)(OEt)2 0 cci2f CN NHMe NP(O)Me2 0 cci2f CN NHMe NP(O)Et2 0 cci2f CN NHMe NP(O)Me(OMe) 0 cci2f CN NHMe NP(O)(OPr)2 0 cci2f CN NHMe NC(O)C(O)H o cci2f CN NHMe NC(O)C(O)Me 0 cci2f CN NHMe NC(O)C(O)OMe 0 cci2f CN NHMe NC(O)C(O)OEt 0 cci2f CN NHMe NC(O)C(O)NH2 0 cci2f CN NHMe NC(O)C(O)OH 0 cci2f CN NHMe NC(NH)NH2 0 94 CC12F CN NHMe NC(NOH)NH2 0 cci2f CN NHMe NC(NH)NHMe 0 cci2f CN NHMe NC(NH)NMe2 0 cci2f CN NHMe NC(NH)OMe 0 cci2f CN NHMe NC(NH)OEt 0 cci2f CN NHEt NCOMe 0 cci2f CN NHEt NCOEt 0 cci2f CN NHEt NCOPr 0 cci2f CN NHEt NCHO O cci2f CN NHEt NCOiPr 0 cci2f CN NHEt NCOtBu 0 cci2f CN NHEt NCOPh 0 cci2f CN NHEt NSO2Me 0 cci2f CN NHEt NSO2Et 0 cci2f CN NHEt NSO2Pr 0 cci2f CN NHEt NSO2Ph 0 cci2f CN NHEt NSO2iPr 0 cci2f CN NHEt nno2 0 cci2f CN NHEt NCOOMe 0 cci2f CN NHEt NCOOEt 0 cci2f CN NHEt NCOOPr 0 cci2f CN NHEt NCOOiPr 0 cci2f CN NHEt NCONHEt 0 cci2f CN NHEt NCONHPr 0 cci2f CN NHEt NCONH2 0 cci2f CN NHEt NCONHMe 0 cci2f CN NHEt NCN 0 cci2f CN NHEt NCOSMe 0 95 CC12F CN NHEt NCOSEt 0 cci2f CN NHEt NCSOMe 0 cci2f CN NHEt NCSOEt 0 cci2f CN NHEt NCSOPr 0 cci2f CN NHEt nso2nh2 0 cci2f CN NHEt NSO2NHMe 0 cci2f CN NHEt NSO2NMe2 0 cci2f CN NHEt NP(O)(OMe)2 0 cci2f CN NHEt NP(O)(OEt)2 0 cci2f CN NHEt NP(O)Me2 0 cci2f CN NHEt NP(O)Et2 0 cci2f CN NHEt NP(O)Me(OMe) 0 cci2f CN NHEt NP(O)(OPr)2 0 cci2f CN NHEt NC(O)C(O)H 0 cci2f CN NHEt NC(O)C(O)Me 0 cci2f CN NHEt NC(O)C(O)OMe 0 cci2f CN NHEt NC(O)C(O)OEt 0 cci2f CN NHEt NC(O)C(O)NH2 0 cci2f CN NHEt NC(O)C(O)OH 0 cci2f CN NHEt NC(NH)NH2 0 cci2f CN NHEt NC(NOH)NH2 0 cci2f CN NHEt NC(NH)NHMe 0 cci2f CN NHEt NC(NH)NMe2 0 cci2f CN NHEt NC(NH)OMe o cci2f CN NHEt NC(NH)OEt 0 cf2ci CN nh2 NCOMe cf2ci CN nh2 NCOEt cf2ci CN nh2 NCOPr 96 CF2C1 CN nh2 NCHO cf2ci CN nh2 NCOiPr cf2ci CN nh2 NCOtBu cf2ci CN nh2 NCOPh cf2ci CN nh2 NSO2Me cf2ci CN nh2 NSO2Et cf2ci CN nh2 NSO2Pr cf2ci CN nh2 NSO2Ph cf2ci CN nh2 NSO2iPr cf2ci CN nh2 NNO2 cf2ci CN nh2 NCOOMe cf2ci CN nh2 NCOOEt cf2ci CN nh2 NCOOPr cf2ci CN nh2 NCOOiPr cf2ci CN nh2 NCONHEt cf2ci CN nh2 NCONHPr cf2ci CN nh2 nconh2 cf2ci CN nh2 NCONHMe cf2ci CN nh2 NCN cf2ci CN nh2 NCOSMe cf2ci CN nh2 NCOSEt cf2ci CN nh2 NCSOMe cf2ci CN nh2 NCSOEt cf2ci CN nh2 NCSOPr cf2ci CN nh2 NSO2NH2 cf2ci CN nh2 NSO2NHMe cf2ci CN nh2 NSO2NMe2 cf2ci CN nh2 NP(O)(OMe)2 97 CF2C1 CN nh2 NP(O)(OEt)2 CF2C1 CN nh2 NP(O)Me2 cf2ci CN nh2 NP(O)Et2 cf2ci CN nh2 NP(O)Me(OMe) cf2ci CN nh2 . NP(O)(OPr)2 cf2ci CN nh2 NC(O)C(O)H cf2ci CN nh2 NC(O)C(O)Me cf2ci CN nh2 NC(O)C(O)OMe cf2ci CN nh2 NC(O)C(O)OEt cf2ci CN nh2 NC(O)C(O)NH2 cf2ci CN nh2 NC(O)C(O)OH cf2ci CN nh2 NC(NH)NH2 cf2ci CN nh2 NC(NOH)NH2 cf2ci CN nh2 NC(NH)NHMe cf2ci CN nh2 NC(NH)NMe2 cf2ci CN nh2 NC(NH)OMe cf2ci CN nh2 NC(NH)OEt cf2ci CN NHMe NCOMe cf2ci CN NHMe NCOEt cf2ci CN NHMe NCOPr cf2ci CN NHMe NCHO cf2ci CN NHMe NCOiPr cf2ci CN NHMe NCOtBu cf2ci CN NHMe NCOPh cf2ci CN NHMe NSO2Me cf2ci CN NHMe NSO2Et cf2ci CN NHMe NSO2Pr cf2ci CN NHMe NSO2Ph 98 CF2C1 CN NHMe NSO2iPr cf2ci CN NHMe nno2 cf2ci CN NHMe NCOOMe cf2ci CN NHMe NCOOEt cf2ci CN NHMe NCOOPr cf2ci CN NHMe NCOOiPr cf2ci CN NHMe NCONHEt cf2ci CN NHMe NCONHPr cf2ci CN NHMe NCONH2 cf2ci CN NHMe NCONHMe cf2ci CN NHMe NCN cf2ci CN NHMe NCOSMe cf2ci CN NHMe NCOSEt cf2ci CN NHMe NCSOMe cf2ci CN NHMe 4 NCSOEt cf2ci CN NHMe NCSOPr cf2ci CN NHMe NSO2NH2 cf2ci CN NHMe NSO2NHMe cf2ci CN NHMe NSO2NMe2 cf2ci CN NHMe NP(O)(OMe)2 cf2ci CN NHMe NP(O)(OEt)2 cf2ci CN NHMe NP(O)Me2 cf2ci CN NHMe NP(O)Et2 cf2ci CN NHMe NP(O)Me(OMe) cf2ci CN NHMe NP(O)(OPr)2 cf2ci CN NHMe NC(O)C(O)H cf2ci CN NHMe NC(O)C(O)Me cf2ci CN NHMe NC(O)C(O)OMe 99 CF2C1 CN NHMe NC(O)C(O)OEt cf2ci CN NHMe NC(O)C(O)NH2 cf2ci CN NHMe NC(O)C(O)OH cf2ci CN . NHMe NC(NH)NH? cf2ci CN NHMe NC(NOH)NH2 cf2ci CN NHMe NC(NH)NHMe cf2ci CN NHMe NC(NH)NMe2 cf2ci CN NHMe NC(NH)OMe cf2ci CN NHMe NC(NH)OEt cf2ci CN NHEt NCOMe cf2ci CN NHEt NCOEt cf2ci CN NHEt NCOPr cf2ci CN NHEt NCHO cf2ci CN NHEt NCOiPr cf2ci CN NHEt NCOtBu cf2ci CN NHEt NCOPh cf2ci CN NHEt NSO2Me cf2ci CN NHEt NSO2Et cf2ci CN NHEt NSO2Pr cf2ci CN NHEt NSO2Ph cf2ci CN NHEt NSO2iPr cf2ci CN NHEt nno2 cf2ci CN NHEt NCOOMe cf2ci CN NHEt NCOOEt cf2ci CN NHEt NCOOPr cf2ci CN NHEt NCOOiPr cf2ci CN NHEt NCONHEt cf2ci CN NHEt NCONHPr 100 CF2C1 CN NHEt NCONH2 CF2C1 CN NHEt NCONHMe cf2ci CN NHEt NCN cf2ci CN NHEt NCOSMe cf2ci CN NHEt NCOSEt cf2ci CN NHEt NCSOMe cf2ci CN NHEt NCSOEt cf2ci CN NHEt NCSOPr cf2ci CN NHEt NSO2NH2 cf2ci CN NHEt NSO2NHMe cf2ci CN NHEt NSO2NMe2 cf2ci CN NHEt NP(O)(OMe)2 cf2ci CN NHEt NP(O)(OEt)2 cf2ci CN NHEt NP(O)Me2 cf2ci CN NHEt NP(O)Et2 cf2ci CN NHEt NP(O)Me(OMe) cf2ci CN NHEt NP(O)(OPr)2 cf2ci CN NHEt NC(O)C(O)H cf2ci CN NHEt NC(O)C(O)Me cf2ci CN NHEt NC(O)C(O)OMe cf2ci CN NHEt NC(O)C(O)OEt cf2ci CN NHEt NC(O)C(O)NH2 cf2ci CN NHEt NC(O)C(O)OH cf2ci CN NHEt NC(NH)NH2 cf2ci CN NHEt NC(NOH)NH2 cf2ci CN NHEt NC(NH)NHMe cf2ci CN NHEt NC(NH)NMe2 cf2ci CN NHEt NC(NH)OMe 101 CF2C1 CN NHEt NC(NH)OEt cf2ci CN nh2 NH 0 cf2ci CN nh2 NCOMe 0 cf2ci CN nh2 NCOEt 0 cf2ci CN nh2 NCOPr 0 cf2ci CN nh2 NCHO 0 cf2ci CN nh2 NCOiPr 0 cf2ci CN nh2 NCOtBu 0 cf2ci CN nh2 NCOPh 0 cf2ci CN nh2 NSO2Me 0 cf2ci CN nh2 NSO2Et O cf2ci CN nh2 NSO2Pr 0 cf2ci CN nh2 NSO2Ph 0 cf2ci CN nh2 NSO2iPr O cf2ci CN nh2 NNO2 0 cf2ci CN nh2 NCOOMe 0 cf2ci CN nh2 NCOOEt 0 cf2ci CN nh2 NCOOPr 0 cf2ci CN nh2 NCOOiPr 0 cf2ci CN nh2 NCONHEt 0 cf2ci CN nh2 NCONHPr 0 cf2ci CN nh2 NCONH2 0 cf2ci CN nh2 NCONHMe 0 cf2ci CN nh2 NCN 0 cf2ci CN nh2 NCOSMe 0 cf2ci CN nh2 NCOSEt 0 cf2ci CN nh2 NCSOMe 0 cf2ci CN nh2 NCSOEt 0 102 CF2C1 CN nh2 NCSOPr 0 cf2ci CN nh2 NSO2NH2 0 cf2ci CN nh2 NSO2NHMe 0 cf2ci CN nh2 NSO2NMe2 0 cf2ci CN nh2 NP(O)(OMe)2 0 cf2ci CN nh2 NP(O)(OEt)2 0 cf2ci CN nh2 NP(O)Me2 0 cf2ci CN nh2 NP(O)Et2 0 cf2ci CN nh2 NP(0)Me(0Me) 0 cf2ci CN nh2 NP(O)(OPr)2 0 cf2ci CN nh2 NC(O)C(O)H 0 cf2ci CN nh2 NC(0)C(0)Me 0 cf2ci CN nh2 NC(0)C(0)0Me 0 cf2ci CN nh2 NC(O)C(O)OEt 0 cf2ci CN nh2 NC(O)C(O)NH2 0 cf2ci CN nh2 NC(O)C(O)OH 0 cf2ci CN nh2 NC(NH)NH2 0 cf2ci CN nh2 NC(N0H)NH2 0 cf2ci CN nh2 NC(NH)NHMe 0 cf2ci CN nh2 NC(NH)NMe2 0 cf2ci CN nh2 NC(NH)0Me 0 cf2ci CN nh2 NC(NH)OEt 0 cf2ci CN NHMe NCOMe 0 cf2ci CN NHMe NCOEt 0 cf2ci CN NHMe NCOPr 0 cf2ci CN NHMe NCHO 0 cf2ci CN NHMe NCOiPr 0 cf2ci CN NHMe NCOtBu 0 103 CF2C1 CN NHMe NCOPh 0 cf2ci CN NHMe NSO2Me 0 cf2ci CN NHMe NSO2Et 0 cf2ci CN NHMe NSO2Pr 0 cf2ci CN NHMe NSO2Ph 0 cf2ci CN NHMe NSO2iPr 0 cf2ci CN NHMe NN02 0 cf2ci CN NHMe NCOOMe 0 cf2ci CN NHMe NCOOEt o cf2ci CN NHMe NCOOPr 0 cf2ci CN NHMe NCOOiPr 0 cf2ci CN NHMe NCONHEt 0 cf2ci CN NHMe NCONHPr 0 cf2ci CN NHMe nconh2 0 cf2ci CN NHMe NCONHMe 0 cf2ci CN NHMe NCN 0 cf2ci CN NHMe NCOSMe 0 cf2ci CN NHMe NCOSEt 0 cf2ci CN NHMe NCSOMe 0 cf2ci CN NHMe NCSOEt 0 cf2ci CN NHMe NCSOPr 0 cf2ci CN NHMe NSO2NH2 0 cf2ci CN NHMe NSO2NHMe 0 cf2ci CN NHMe NSO2NMe2 0 cf2ci CN NHMe NP(O)(OMe)2 . 0 cf2ci CN NHMe NP(O)(OEt)2 0 cf2ci CN NHMe NP(O)Me2 0 cf2ci CN NHMe NP(O)Et2 o 104 CF2C1 CN NHMe NP(O)Me(OMe) 0 cf2ci CN NHMe NP(O)(OPr)2 0 cf2ci CN NHMe NC(O)C(O)H 0 cf2ci CN NHMe NC(O)C(O)Me O cf2ci CN NHMe NC(O)C(O)OMe O cf2ci CN NHMe NC(O)C(O)OEt 0 cf2ci CN NHMe NC(O)C(O)NH2 0 cf2ci CN NHMe NC(O)C(O)OH 0 cf2ci CN NHMe NC(NH)NH2 0 cf2ci CN NHMe NC(NOH)NH2 O cf2ci CN NHMe NC(NH)NHMe O cf2ci CN NHMe NC(NH)NMe2 0 cf2ci CN NHMe NC(NH)OMe O cf2ci CN NHMe NC(NH)0Et 0 cf2ci CN NHEt NCOMe 0 cf2ci CN NHEt NCOEt 0 cf2ci CN NHEt NCOPr O cf2ci CN NHEt NCHO 0 cf2ci CN NHEt NCOiPr 0 cf2ci CN NHEt NCOtBu 0 cf2ci CN NHEt NCOPh 0 cf2ci CN NHEt NSO2Me 0 cf2ci CN NHEt NSO2Et 0 cf2ci CN NHEt NSO2Pr 0 cf2ci CN NHEt NSO2Ph 0 cf2ci CN NHEt NSO2iPr 0 cf2ci CN NHEt nno2 0 cf2ci CN NHEt NCOOMe o 105 CF2C1 CN NHEt NCOOEt 0 cf2ci CN NHEt NCOOPr 0 cf2ci CN NHEt NCOOiPr 0 cf2ci CN NHEt NCONHEt 0 cf2ci CN NHEt NCONHPr 0 cf2ci CN NHEt NCONH2 0 cf2ci CN NHEt NCONHMe 0 cf2ci CN NHEt NCN O cf2ci CN NHEt NCOSMe 0 cf2ci CN NHEt NCOSEt 0 cf2ci CN NHEt NCSOMe 0 cf2ci CN NHEt NCSOEt 0 cf2ci CN NHEt NCSOPr 0 cf2ci CN NHEt NSO2NH2 0 cf2ci CN NHEt NSO2NHMe 0 cf2ci CN NHEt NSO2NMe2 0 cf2ci CN NHEt NP(O)(OMe)2 0 cf2ci CN NHEt NP(O)(OEt)2 0 cf2ci CN NHEt NP(O)Me2 0 cf2ci CN NHEt NP(O)Et2 0 cf2ci CN NHEt NP(O)Me(OMe) 0 cf2ci CN NHEt NP(O)(OPr)2 0 cf2ci CN NHEt NC(O)C(O)H 0 cf2ci CN NHEt NC(O)C(O)Me 0 cf2ci CN NHEt NC(0)C(0)0Me 0 cf2ci CN NHEt NC(O)C(O)OEt 0 cf2ci CN NHEt NC(O)C(O)NH2 0 cf2ci CN NHEt NC(O)C(O)OH 0 106

CF2C1 CN NHEt NC(NH)NH2 0 cf2ci CN NHEt NC(NOH)NH2 0 cf2ci CN NHEt NC(NH)NHMe 0 cf2ci CN NHEt NC(NH)NMe2 0 cf2ci CN NHEt NC(NH)OMe o cf2ci CN NHEt NC(NH)OEt 0 cf3 CN H NCOMe cf3 CN H NCOEt cf3 CN H NCOPr cf3 CN H NCHO cf3 CN H NCOiPr cf3 CN H NCOtBu cf3 CN H NCOPh cf3 CN H NSO2Me cf3 CN H NSO2Et cf3 CN H NSO2Pr cf3 CN H NSO2Ph cf3 CN H NSO2iPr cf3 CN H NNO2 cf3 CN H NCOOMe cf3 CN H NCOOEt cf3 CN H NCOOPr cf3 CN H NCOOiPr cf3 CN H NCONHEt cf3 CN H NCONHPr cf3 CN H NC0NH2 cf3 CN H NCONHMe cf3 CN H NCN 107 cf3 CN H NCOSMe cf3 CN H NCOSEt cf3 CN H NCSOMe cf3 CN H NCSOEt cf3 CN H NCSOPr cf3 CN H NSO2NH2 cf3 CN H NSO2NHMe cf3 CN H NSO2NMe2 cf3 CN H NP(O)(OMe)2 cf3 CN H NP(O)(OEt)2 cf3 CN H NP(O)Me2 cf3 CN H NP(O)Et2 cf3 CN H NP(O)Me(OMe) cf3 CN H NP(O)(OPr)2 cf3 CN H NC(O)C(O)H cf3 CN H NC(O)C(O)Me cf3 CN H NC(O)C(O)OMe cf3 CN H NC(O)C(O)OEt cf3 CN H NC(O)C(O)NH2 cf3 CN H NC(O)C(O)OH cf3 CN H NC(NH)NH2 cf3 CN H NC(NOH)NH2 cf3 CN H NC(NH)NHMe cf3 CN H NC(NH)NMe2 cf3 CN H NC(NH)0Me cf3 CN H NC(NH)OEt cf3 CN H NH cf3 CN H NCOMe 108 cf3 CN H NCOEt cf3 CN H NCOPr cf3 CN H NCHO cf3 CN H NCOiPr cf3 CN H NCOtBu cf3 CN H NCOPh cf3 CN H NS02Me cf3 CN H NSO2Et cf3 CN H NSO2Pr cf3 CN H NSO2Ph cf3 CN H NSO2iPr cf3 CN H nno2 cf3 CN H NCOOMe cf3 CN H NCOOEt cf3 CN H NCOOPr cf3 CN H NCOOiPr cf3 CN H NCONHEt cf3 CN H NCONHPr cf3 CN H NC0NH2 cf3 CN H NCONHMe cf3 CN H NCN cf3 CN H NCOSMe cf3 CN H NCOSEt cf3 CN H NCSOMe cf3 CN H NCSOEt cf3 CN H NCSOPr cf3 CN H NSO2NH2 cf3 CN H NSO2NHMe ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο 109 cf3 CN H NSO2NMe2 0 cf3 CN H NP(O)(OMe)2 0 cf3 CN H NP(O)(OEt)2 0 cf3 CN H NP(O)Me2 0 cf3 CN H NP(O)Et2 0 cf3 CN H NP(O)Me(OMe) 0 cf3 CN H NP(O)(OPr)2 0 cf3 CN H NC(O)C(O)H 0 cf3 CN H NC(O)C(O)Me O cf3 CN H NC(O)C(O)OMe 0 cf3 CN H NC(O)C(O)OEt 0 cf3 CN H NC(O)C(O)NH2 0 cf3 CN H NC(O)C(O)OH 0 cf3 CN H NC(NH)NH2 0 cf3 CN H NC(NOH)NH2 0 cf3 CN H NC(NH)NHMe 0 cf3 CN H NC(NH)NMe2 0 cf3 CN H NC(NH)OMe 0 cf3 CN H NC(NH)OEt 0 cf3 CN Me NCOMe cf3 CN Me NCOEt cf3 CN Me NCOPr cf3 CN Me NCHO cf3 CN Me NCOiPr cf3 CN Me NCOtBu cf3 CN Me NCOPh cf3 CN Me NSO2Me cf3 CN Me NSO2Et 110

cf3 CN Me NSO2Pr cf3 CN Me NSO2Ph cf3 CN Me NSO2iPr cf3 CN Me nno2 cf3 CN Me NCOOMe cf3 CN Me NCOOEt cf3 CN Me NCOOPr cf3 CN Me NCOOiPr cf3 CN Me NCONHEt cf3 CN Me NCONHPr cf3 CN Me NCOH cf3 CN Me NCONHMe cf3 CN Me NCN cf3 CN Me NCOSMe cf3 CN Me NCOSEt cf3 CN Me NCSOMe cf3 CN Me NCSOEt cf3 CN Me NCSOPr cf3 CN Me NSO2H cf3 CN Me NSO2NHMe cf3 CN Me NSO2NMe2 cf3 CN Me NP(O)(OMe)2 cf3 CN Me NP(O)(OEt)2 cf3 CN Me NP(O)Me2 cf3 CN Me NP(O)Et2 cf3 CN Me NP(O)Me(OMe) cf3 CN Me NP(O)(OPr)2 cf3 CN Me NC(O)C(O)H

Ill CF3 CN Me NC(O)C(O)Me cf3 CN Me NC(O)C(O)OMe cf3 CN Me NC(O)C(O)OEt cf3 CN Me NC(O)C(O)NH2 cf3 CN Me NC(O)C(O)OH cf3 CN Me NC(NH)H cf3 CN Me NC(NOH)H cf3 CN Me NC(NH)NHMe cf3 CN Me NC(NH)NMe2 cf3 CN Me NC(NH)OMe cf3 CN Me NC(NH)OEt cf3 CN Me NH 0 cf3 CN Me NCOMe 0 cf3 CN Me NCOEt O cf3 CN Me NCOPr 0 cf3 CN Me NCHO 0 cf3 CN Me NCOiPr O cf3 CN Me NCOtBu 0 cf3 CN Me NCOPh 0 cf3 CN Me NSO2Me O cf3 CN Me NSO2Et 0 cf3 CN Me NSO2Pr 0 cf3 CN Me NSO2Ph 0 cf3 CN Me NSO2iPr 0 cf3 CN Me NNO2 0 cf3 CN Me NCOOMe 0 cf3 CN Me NCOOEt 0 cf3 CN Me NCOOPr 0 112 cf3 CN Me NCOOiPr 0 cf3 CN Me NCONHEt 0 cf3 CN Me NCONHPr 0 cf3 CN Me nconh2 0 cf3 CN Me NCONHMe 0 cf3 CN Me NCN 0 cf3 CN Me NCOSMe 0 cf3 CN Me NCOSEt 0 cf3 CN Me NCSOMe 0 cf3 CN Me NCSOEt o cf3 CN Me NCSOPr 0 cf3 CN Me NSO2NH2 0 cf3 CN Me NSO2NHMe 0 cf3 CN Me NSO2NMe2 0 cf3 CN Me NP(O)(OMe)2 0 cf3 CN Me NP(O)(OEt)2 0 cf3 CN Me NP(O)Me2 0 cf3 CN Me NP(O)Et2 0 cf3 CN Me NP(O)Me(OMe) 0 cf3 CN Me NP(O)(OPr)2 0 cf3 CN Me NC(O)C(O)H 0 cf3 CN Me NC(O)C(O)Me 0 cf3 CN Me NC(O)C(O)OMe 0 cf3 CN Me NC(O)C(O)OEt 0 cf3 CN Me NC(O)C(O)NH2 0 cf3 CN Me NC(O)C(O)OH 0 cf3 CN Me NC(NH)NH2 0 cf3 CN Me NC(NOH)NH2 0 113 cf3 CN Me NC(NH)NHMe cf3 CN Me NC(NH)NMe2 cf3 CN Me NC(NH)OMe cf3 CN Me NC(NH)OEt cf3 CN Cl NCOMe cf3 CN Cl NCOEt cf3 CN Cl NCOPr cf3 CN Cl NCHO cf3 CN Cl NCOiPr cf3 CN Cl NCOtBu cf3 CN Cl NCOPh cf3 CN Cl NSO2Me cf3 CN Cl NSO2Et cf3 CN Cl NSO2Pr cf3 CN Cl NSO2Ph cf3 CN Cl NSO2iPr cf3 CN Cl nno2 cf3 CN Cl NCOOMe cf3 CN Cl NCOOEt cf3 CN Cl NCOOPr cf3 CN Cl NCOOiPr cf3 CN Cl NCONHEt cf3 CN Cl NCONHPr cf3 CN Cl NCOH cf3 CN Cl NCONHMe cf3 CN Cl NCN cf3 CN Cl NCOSMe cf3 CN Cl NCOSEt 114

cf3 CN Cl NCSOMe cf3 CN Cl NCSOEt cf3 CN Cl NCSOPr cf3 CN Cl NSO2H cf3 CN Cl NSO2NHMe cf3 CN Cl NSO2NMe2 cf3 CN Cl NP(O)(OMe)2 cf3 CN Cl NP(O)(OEt)2 cf3 CN Cl NP(O)Me2 cf3 CN Cl NP(O)Et2 cf3 CN Cl NP(O)Me(OMe) cf3 CN Cl NP(O)(OPr)2 cf3 CN Cl NC(O)C(O)H cf3 CN Cl NC(O)C(O)Me cf3 CN Cl NC(O)C(O)OMe cf3 CN Cl NC(O)C(O)OEt cf3 CN Cl NC(O)C(O)NH2 cf3 CN Cl NC(O)C(O)OH cf3 CN Cl NC(NH)H cf3 CN Cl NC(NOH)H cf3 CN Cl NC(NH)NHMe cf3 CN Cl NC(NH)NMe2 cf3 CN Cl NC(NH)OMe cf3 CN Cl NC(NH)OEt cf3 CN Cl NCOMe cf3 CN Cl NCOEt cf3 CN Cl NCOPr cf3 CN Cl NCHO 115 CF3 CN Cl NCOiPr 0 cf3 CN Cl NCOtBu 0 cf3 CN Cl NCOPh 0 CF3 CN Cl NSO2Me 0 cf3 CN Cl NSO2Et 0 cf3 CN Cl NSO2Pr 0 cf3 CN Cl NSO2Ph 0 cf3 CN Cl NSO2iPr 0 cf3 CN Cl nno2 0 cf3 CN Cl NCOOMe 0 cf3 CN Cl NCOOEt 0 cf3 CN Cl NCOOPr 0 cf3 CN Cl NCOOiPr 0 cf3 CN Cl NCONHEt 0 cf3 CN Cl NCONHPr 0 cf3 CN Cl nconh2 0 cf3 CN Cl NCONHMe 0 cf3 CN Cl NCN 0 cf3 CN Cl NCOSMe 0 cf3 CN Cl NCOSEt 0 cf3 CN Cl NCSOMe 0 cf3 CN Cl NCSOEt 0 cf3 CN Cl NCSOPr 0 cf3 CN Cl nso2nh2 0 cf3 CN Cl NSO2NHMe 0 cf3 CN Cl NSO2NMe2 0 cf3 CN Cl NP(O)(OMe)2 0 cf3 CN Cl NP(O)(OE02 0 116 cf3 CN Cl NP(O)Me2 0 cf3 CN Cl NP(O)Et2 0 cf3 CN Cl NP(O)Me(OMe) 0 cf3 CN Cl NP(O)(OPr)2 0 cf3 CN Cl NC(O)C(O)H 0 cf3 CN Cl NC(O)C(O)Me 0 cf3 CN Cl NC(O)C(O)OMe 0 cf3 CN Cl NC(O)C(O)OEt 0 cf3 CN Cl NC(O)C(O)NH2 0 cf3 CN Cl NC(O)C(O)OH 0 cf3 CN Cl NC(NH)NH2 0 cf3 CN Cl NC(NOH)NH2 0 cf3 CN Cl NC(NH)NHMe 0 cf3 CN Cl NC(NH)NMe2 0 cf3 CN Cl NC(NH)OMe 0 cf3 CN Cl NC(NH)OEt 0 cf3 CN SMe NCOMe cf3 CN SMe NCOEt cf3 CN SMe NCOPr cf3 CN SMe NCHO cf3 CN SMe NCOiPr cf3 CN SMe NCOtBu cf3 CN . SMe NCOPh cf3 CN SMe NSO2Me cf3 CN SMe NSO2Et cf3 CN SMe NSO2Pr cf3 CN SMe NSO2Ph cf3 CN SMe NSO2iPr 117 cf3 CN SMe nno2 cf3 CN SMe NCOOMe cf3 CN SMe NCOOEt cf3 CN SMe NCOOPr cf3 CN SMe NCOOiPr cf3 CN SMe NCONHEt cf3 CN SMe NCONHPr cf3 CN SMe NCOH cf3 CN SMe NCONHMe cf3 CN SMe NCN cf3 CN SMe NCOSMe cf3 CN SMe NCOSEt cf3 CN SMe NCSOMe cf3 CN SMe NCSOEt cf3 CN SMe NCSOPr cf3 CN SMe NSO2H cf3 CN SMe NSO2NHMe cf3 CN . SMe NSO2NMe2 cf3 CN SMe NP(O)(OMe)2 cf3 CN SMe NP(O)(OEt)2 cf3 CN SMe NP(O)Me2 cf3 CN SMe NP(O)Et2 cf3 CN SMe NP(O)Me(OMe) cf3 CN SMe NP(O)(OPr)2 cf3 CN SMe NC(O)C(O)H cf3 CN SMe NC(O)C(O)Me cf3 CN SMe NC(O)C(O)OMe cf3 CN SMe NC(O)C(O)OEt 118

cf3 CN SMe NC(O)C(O)NH2 cf3 CN SMe NC(O)C(O)OH cf3 CN SMe NC(NH)H cf3 CN SMe NC(NOH)H cf3 CN SMe NC(NH)NHMe cf3 CN SMe NC(NH)NMe2 cf3 CN SMe NC(NH)OMe cf3 CN SMe NC(NH)OEt cf3 H nh2 NCOMe cf3 H nh2 NCOEt cf3 H nh2 NCOPr cf3 H nh2 NCHO cf3 H nh2 NCOiPr cf3 H nh2 NCOtBu cf3 H nh2 NCOPh cf3 H nh2 NSO2Me cf3 H nh2 NSO2Et cf3 H nh2 NSO2Pr cf3 H nh2 NSO2Ph cf3 H nh2 NSO2iPr cf3 H nh2 nno2 cf3 H nh2 NCOOMe cf3 H nh2 NCOOEt cf3 H nh2 NCOOPr cf3 H nh2 NCOOiPr cf3 H nh2 NCONHEt cf3 H nh2 NCONHPr cf3 H nh2 NCOH 119 cf3 H nh2 NCONHMe cf3 H nh2 NCN cf3 H nh2 NCOSMe cf3 H nh2 NCOSEt cf3 H nh2 NCSOMe cf3 H nh2 NCSOEt cf3 H nh2 NCSOPr cf3 H nh2 NSO2H cf3 H nh2 NSO2NHMe cf3 H nh2 NSO2NMe2 cf3 H nh2 NP(O)(OMe)2 cf3 H nh2 NP(O)(OEt)2 cf3 H nh2 NP(O)Me2 cf3 H nh2 NP(O)Et2 cf3 H nh2 NP(O)Me(OMe) cf3 H nh2 NP(O)(OPr)2 cf3 H nh2 NC(O)C(O)H cf3 H nh2 NC(O)C(O)Me cf3 H nh2 NC(O)C(O)OMe cf3 H nh2 NC(O)C(O)OEt cf3 H nh2 NC(O)C(O)NH2 cf3 H nh2 NC(O)C(O)OH cf3 H nh2 NC(NH)H cf3 H nh2 NC(NOH)H cf3 H nh2 NC(NH)NHMe cf3 H nh2 NC(NH)NMe2 cf3 H nh2 NC(NH)OMe cf3 H nh2 NC(NH)OEt 120

CF3 Me NH, NCOMe cf3 Me nh. NCOEt cf3 Me nh2 NCOPr cf3 Me nh2 NCHO cf3 Me nh2 NCOiPr cf3 Me nh2 NCOtBu cf3 Me nh2 NCOPh cf3 Me nh2 NSO2Me cf3 Me nh2 NSO2Et cf3 Me nh2 NSO2Pr cf3 Me nh2 NSO2Ph cf3 Me nh2 NSO2iPr cf3 Me nh2 NN02 cf3 Me nh2 NCOOMe cf3 Me nh2 NCOOEt cf3 Me nh2 NCOOPr cf3 Me nh2 NCOOiPr cf3 Me nh2 NCONHEt cf3 Me nh2 NCONHPr cf3 Me nh2 NCOH cf3 Me nh2 NCONHMe cf3 Me nh2 NCN cf3 Me nh2 NCOSMe cf3 Me nh2 NCOSEt cf3 Me nh2 NCSOMe cf3 Me nh2 NCSOEt cf3 Me nh2 NCSOPr cf3 Me nh2 NSO2H 121 cf3 Me nh2 NSO2NHMe cf3 Me nh2 NSO2NMe2 cf3 Me nh2 NP(O)(OMe)2 cf3 Me nh2 NP(O)(OEt)2 cf3 Me nh2 NP(O)Me2 cf3 Me nh2 NP(O)Et2 cf3 Me nh2 NP(O)Me(OMe) cf3 Me nh2 NP(O)(OPr)2 cf3 Me nh2 NC(O)C(O)H cf3 Me nh2 NC(O)C(O)Me cf3 Me nh2 NC(O)C(O)OMe cf3 Me nh2 NC(O)C(O)OEt cf3 Me nh2 NC(O)C(O)NH2 cf3 Me nh2 NC(O)C(O)OH cf3 Me nh2 NC(NH)H cf3 Me nh2 NC(NOH)H cf3 Me nh2 NC(NH)NHMe cf3 Me nh2 NC(NH)NMe2 cf3 Me nh2 NC(NH)OMe cf3 Me nh2 NC(NH)OEt cf3 H H NCOMe cf3 H H NCOEt cf3 H H NCOPr cf3 H H NCHO cf3 H H NCOiPr cf3 H H NCOtBu cf3 H H NCOPh cf3 H H NSO2Me 122 cf3 H H NSO2Et cf3 H H NSO2Pr cf3 H H NSO2Ph cf3 H H NSO2iPr cf3 H H NNO2 cf3 H H NCOOMe cf3 H H NCOOEt cf3 H H NCOOPr cf3 H H NCOOiPr cf3 H H NCONHEt cf3 H H NCONHPr cf3 H H NCOH cf3 H H NCONHMe cf3 H H NCN cf3 H H NCOSMe cf3 H H NCOSEt cf3 H H NCSOMe cf3 H H NCSOEt cf3 H H NCSOPr cf3 H H NSO2H cf3 H H NSO2NHMe cf3 H H NSO2NMe2 cf3 H H NP(O)(OMe)2 cf3 H H NP(O)(OEt)2 cf3 H H NP(O)Me2 cf3 H H NP(O)Et2 cf3 H H NP(O)Me(OMe) cf3 H H NP(O)(OPr)2 123 cf3 H H NC(O)C(O)H cf3 H H NC(O)C(O)Me cf3 H H NC(O)C(O)OMe cf3 H H NC(O)C(O)OEt cf3 H H NC(O)C(O)NH2 cf3 H H NC(O)C(O)OH cf3 H H NC(NH)H cf3 H H NC(NOH)H cf3 H H NC(NH)NHMe cf3 H H NC(NH)NMe2 cf3 H H NC(NH)OMe cf3 H H NC(NH)OEt cf3 Me H NCOMe cf3 Me H NCOEt cf3 Me H NCOPr cf3 Me H NCHO cf3 Me H NCOiPr cf3 Me H NCOtBu cf3 Me H NCOPh cf3 Me H NSO2Me cf3 Me H NSO2Et cf3 Me H NSO2Pr cf3 Me H NSO2Ph cf3 Me H NSO2iPr cf3 Me H nno2 cf3 Me H NCOOMe cf3 Me H NCOOEt cf3 Me H NCOOPr 124

cf3 Me H NCOOiPr cf3 Me H NCONHEt cf3 Me H NCONHPr cf3 Me H NCOH cf3 Me H NCONHMe cf3 Me H NCN cf3 Me H NCOSMe cf3 Me H NCOSEt cf3 Me H NCSOMe cf3 Me H NCSOEt cf3 Me ! H NCSOPr cf3 Me H NSO2H cf3 Me H NSO2NHMe cf3 Me H NSO2NMe2 cf3 Me H NP(O)(OMe)2 cf3 Me H NP(O)(OEt)2 cf3 Me H NP(O)Me2 cf3 Me H NP(O)Et2 cf3 Me H NP(O)Me(OMe) cf3 Me H NP(O)(OPr)2 cf3 Me H NC(O)C(O)H cf3 Me H NC(O)C(O)Me cf3 Me H NC(O)C(O)OMe cf3 Me H NC(O)C(O)OEt cf3 Me H NC(O)C(O)NH2 cf3 Me H NC(O)C(O)OH cf3 Me H NC(NH)H cf3 Me H NC(NOH)H 125 CF3 Me H NC(NH)NHMe cf3 Me H NC(NH)NMe2 cf3 Me H NC(NH)OMe cf3 Me H NC(NH)OEt cf3 H Cl NCOMe cf3 H Cl NCOEt cf3 H Cl NCOPr cf3 H Cl NCHO cf3 H Cl NCOiPr cf3 H Cl NCOtBu cf3 H Cl NCOPh cf3 H Cl NSO2Me cf3 H Cl NSO2Et cf3 H Cl NSO2Pr cf3 H Cl NSO2Ph cf3 H Cl NSO2iPr cf3 H Cl NNO2 cf3 H Cl NCOOMe cf3 H Cl NCOOEt cf3 H Cl NCOOPr cf3 H Cl NCOOiPr cf3 H Cl NCONHEt cf3 H Cl NCONHPr cf3 H Cl NCOH cf3 H Cl NCONHMe cf3 H Cl NCN cf3 H Cl NCOSMe cf3 H Cl NCOSEt 126

cf3 H Cl NCSOMe cf3 H Cl NCSOEt cf3 H Cl NCSOPr cf3 H Cl NSO2H cf3 H Cl NSO2NHMe cf3 H Cl NSO2NMe2 cf3 H Cl NP(O)(OMe)2 cf3 H Cl NP(O)(OEt)2 cf3 H Cl NP(O)Me2 cf3 H Cl NP(O)Et2 cf3 H Cl NP(O)Me(OMe) cf3 H Cl NP(O)(OPr)2 cf3 H Cl NC(O)C(O)H cf3 H Cl NC(O)C(O)Me cf3 H Cl NC(O)C(O)OMe cf3 H Cl NC(O)C(O)OEt cf3 H Cl NC(O)C(O)NH2 cf3 H Cl NC(O)C(O)OH cf3 H Cl NC(NH)H cf3 H Cl NC(NOH)H cf3 H Cl NC(NH)NHMe cf3 H Cl NC(NH)NMe2 cf3 H Cl NC(NH)OMe cf3 H Cl NC(NH)OEt cf3 Me Cl NCOMe cf3 Me Cl NCOEt cf3 Me Cl NCOPr cf3 Me Cl NCHO 127 cf3 Me Cl NCOiPr cf3 Me Cl NCOtBu cf3 Me Cl NCOPh cf3 Me Cl NSO2Me cf3 Me Cl NSO2Et cf3 Me Cl NSO2Pr cf3 Me Cl NSO2Ph cf3 Me Cl NSO2iPr cf3 Me Cl nno2 cf3 Me Cl NCOOMe cf3 Me Cl NCOOEt cf3 Me Cl NCOOPr cf3 Me Cl NCOOiPr cf3 Me Cl NCONHEt cf3 Me Cl NCONHPr cf3 Me Cl NCOH cf3 Me Cl NCONHMe cf3 Me Cl NCN cf3 Me Cl NCOSMe cf3 Me Cl NCOSEt cf3 Me Cl NCSOMe cf3 Me Cl NCSOEt cf3 Me Cl NCSOPr cf3 Me Cl NSO2H cf3 Me Cl NSO2NHMe cf3 Me Cl NSO2NMe2 cf3 Me Cl NP(O)(OMe)2 cf3 Me Cl NP(O)(OEt)2 128 cf3 Me Cl NP(O)Me2 cf3 Me Cl NP(O)Et2 cf3 Me Cl NP(O)Me(OMe) cf3 Me Cl NP(O)(OPr)2 cf3 Me Cl NC(O)C(O)H cf3 Me Cl NC(O)C(O)Me cf3 Me Cl NC(O)C(O)OMe cf3 Me Cl NC(O)C(O)OEt cf3 Me Cl NC(O)C(O)NH2 cf3 Me Cl NC(O)C(O)OH cf3 Me Cl NC(NH)H cf3 Me Cl NC(NOH)H cf3 Me Cl NC(NH)NHMe cf3 Me Cl NC(NH)NMe2 cf3 Me Cl NC(NH)OMe cf3 Me Cl NC(NH)OEt Me H nh2 NCOMe Me H nh2 NCOEt Me H nh2 NCOPr Me H nh2 NCHO Me H nh2 NCOiPr Me H nh2 NCOtBu Me H nh2 NCOPh Me H nh2 NSO2Me Me H nh2 NSO2Et Me H nh2 NSO2Pr Me H nh2 NSO2Ph Me H nh2 NSO2iPr 129

Me H nh2 nno2 Me H nh2 NCOOMe Me H nh2 NCOOEt Me H nh2 NCOOPr Me H nh2 NCOOiPr Me H nh2 NCONHEt Me H nh2 NCONHPr Me H nh2 NCOH Me H nh2 NCONHMe Me H nh2 NCN Me H nh2 NCOSMe Me H nh2 NCOSEt Me H nh2 NCSOMe Me H nh2 NCSOEt Me H nh2 NCSOPr Me H nh2 NSO2H Me H nh2 NSO2NHMe Me H nh2 NSO2NMe2 Me H nh2 NP(O)(OMe)2 Me H nh2 NP(O)(OEt)2 Me H nh2 NP(O)Me2 Me H nh2 NP(O)Et2 Me H nh2 NP(O)Me(OMe) Me H nh2 NP(O)(OPr)2 Me H nh2 NC(O)C(O)H Me H nh2 NC(O)C(O)Me Me H nh2 NC(O)C(O)OMe Me H nh2 NC(O)C(O)OEt 130

Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H '.nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 Me H nh2 NC(O)C(O)NH2

NC(O)C(O)OH

NC(NH)H

NC(NOH)H NC(NH)NHMe NC(NH)NMe2 NC(NH)0Me NC(NH)OEt

NH O NCOMe 0

NCOEt O

NCOPr O

NCHO O

NCOiPr O

NCOtBu O

NCOPh O

NSO2Me O

NSO2Et O

NSO2Pr O

NSO2Ph O

NSO2iPr O

NN02 O

NCOOMe O

NCOOEt O

NCOOPr O

NCOOiPr O

NCONHEt O

NCONHPr O 131

Me H nh2 NCOH 0 Me H nh2 NCONHMe 0 Me H nh2 NCN 0 Me H nh2 NCOSMe 0 Me H nh2 NCOSEt O Me H nh2 NCSOMe 0 Me H nh2 NCSOEt 0 Me H nh2 NCSOPr 0 Me H nh2 NSO2H 0 Me H nh2 NSO2NHMe 0 Me H nh2 NSO2NMe2 0 Me H nh2 NP(O)(OMe)2 0 Me H nh2 NP(O)(OEt)2 0 Me H nh2 NP(O)Me2 0 Me H nh2 NP(O)Et2 0 Me H nh2 NP(O)Me(OMe) 0 Me H nh2 NP(O)(OPr)2 0 Me H nh2 NC(O)C(O)H 0 Me H nh2 NC(O)C(O)Me 0 Me H nh2 NC(O)C(O)OMe 0 Me H nh2 NC(O)C(O)OEt 0 Me H nh2 NC(O)C(O)NH2 0 Me H nh2 NC(O)C(O)OH 0 Me H nh2 NC(NH)H 0 Me H nh2 NC(NOH)H 0 Me H nh2 NC(NH)NHMe 0 Me H nh2 NC(NH)NMe2 0 Me H nh2 NC(NH)OMe 0 132

Me H nh2 NC(NH)OEt Me Me nh2 NCOMe Me Me nh2 NCOEt Me Me nh2 NCOPr Me Me nh2 NCHO Me Me nh2 NCOiPr Me Me nh2 NCOtBu Me Me nh2 NCOPh Me Me nh2 NSO2Me Me Me nh2 NSO2Et Me Me nh2 NSO2Pr Me Me nh2 NSO2Ph Me Me nh2 NSO2iPr Me Me nh2 nno2 Me Me nh2 NCOOMe Me Me nh2 NCOOEt Me Me nh2 NCOOPr Me Me nh2 NCOOiPr Me Me nh2 NCONHEt Me Me nh2 NCONHPr Me Me nh2 NCOH Me Me nh2 NCONHMe Me Me nh2 NCN Me Me nh2 NCOSMe Me Me nh2 NCOSEt Me Me nh2 NCSOMe Me Me nh2 NCSOEt Me Me nh2 NCSOPr 133

Me Me nh2 nso2h Me Me nh2 NSO,NHMe Me Me nh2 NSO2NMe2 Me Me nh2 NP(O)(OMe)2 Me Me nh2 NP(O)(OEt)2 Me Me nh2 NP(O)Me2 Me Me nh2 NP(O)Et2 Me Me nh2 NP(O)Me(OMe) Me Me nh2 NP(O)(OPr)2 Me Me nh2 NC(O)C(O)H Me Me nh2 NC(O)C(O)Me Me Me nh2 NC(O)C(O)OMe Me Me nh2 NC(O)C(O)OEt Me Me nh2 NC(O)C(O)NH2 Me Me nh2 NC(O)C(O)OH Me Me nh2 NC(NH)H Me Me nh2 NC(NOH)H Me Me nh2 NC(NH)NHMe Me Me nh2 NC(NH)NMe2 Me Me nh2 NC(NH)OMe Me Me nh2 NC(NH)OEt Me Me nh2 NH 0 Me Me nh2 NCOMe 0 Me Me nh2 NCOEt 0 Me Me nh2 NCOPr 0 Me Me nh2 NCHO 0 Me Me nh2 NCOiPr 0 Me Me nh2 NCOtBu 0 134

Me Me nh2 NCOPh 0 Me Me nh2 NSO2Me 0 Me Me nh2 NSO2Et 0 Me Me nh2 NSO2Pr 0 Me Me nh2 NSO2Ph 0 Me Me nh2 NSO2iPr 0 Me Me nh2 NNO2 0 Me Me nh2 NCOOMe 0 Me Me nh2 NCOOEt 0 Me Me nh2 NCOOPr 0 Me Me nh2 NCOOiPr 0 Me Me nh2 NCONHEt 0 Me Me nh2 NCONHPr 0 Me Me nh2 NCOH 0 Me Me nh2 NCONHMe 0 Me Me nh2 NCN 0 Me Me nh2 NCOSMe 0 Me Me nh2 NCOSEt 0 Me Me nh2 NCSOMe 0 Me Me nh2 NCSOEt 0 Me Me nh2 NCSOPr 0 Me Me nh2 NSO2H 0 Me Me nh2 NSO2NHMe 0 Me Me nh2 NSO2NMe2 0 Me Me nh2 NP(O)(OMe)2 0 Me Me nh2 NP(O)(OEt)2 0 Me Me nh2 NP(O)Me2 0 Me Me nh2 NP(O)Et2 0 135

Me Me nh2 NP(O)Me(OMe) 0 Me Me nh2 NP(O)(OPr)2 0 Me Me nh2 NC(O)C(O)H 0 Me Me nh2 NC(O)C(O)Me 0 Me Me nh2 NC(O)C(O)OMe 0 Me Me nh2 NC(O)C(O)OEt 0 Me Me nh2 NC(O)C(O)NH2 0 Me Me nh2 NC(O)C(O)OH 0 Me Me nh2 NC(NH)H 0 Me Me nh2 NC(NOH)H 0 Me Me nh2 NC(NH)NHMe 0 Me Me nh2 NC(NH)NMe2 0 Me Me nh2 NC(NH)OMe 0 Me Me nh2 NC(NH)OEt 0 Me H H NCOMe Me H H NCOEt Me H H NCOPr Me H H NCHO Me H H NCOiPr Me H H NCOtBu Me H H NCOPh Me H H NSO2Me Me H H NSO2Et Me H H NSO2Pr Me H H NSO2Ph Me H H NSO2iPr Me H H NNO2 Me H H NCOOMe 136

Me H H NCOOEt Me H H NCOOPr Me H H NCOOiPr Me H H NCONHEt Me H H NCONHPr Me H H NCOH Me H H NCONHMe Me H H NCN Me H H NCOSMe Me H H NCOSEt Me H H NCSOMe Me H H NCSOEt Me H H NCSOPr Me H H NSO2H Me H H NSO2NHMe Me H H NSO2NMe2 Me H H NP(O)(OMe)2 Me H H NP(O)(OEt)2 Me H H NP(O)Me2 Me H H NP(O)Et2 Me H H NP(O)Me(OMe) Me H H NP(O)(OPr)2 Me H H NC(O)C(O)H Me H H NC(O)C(O)Me Me H H NC(O)C(O)OMe Me H H NC(O)C(O)OEt Me H H NC(O)C(O)NH2 Me H H NC(O)C(O)OH 137

Me H H NC(NH)H Me H H NC(NOH)H Me H H NC(NH)NHMe Me H H NC(NH)NMe2 Me H H NC(NH)OMe Me H H NC(NH)OEt Me H Me NCOMe Me H Me NCOEt Me H Me NCOPr Me H Me NCHO Me H Me NCOiPr Me H Me NCOtBu Me H Me NCOPh Me H Me NSO2Me Me H Me NSO2Et Me H Me NSO2Pr Me H Me NSO2Ph Me H Me NSO2iPr Me H Me NNO2 Me H Me NCOOMe Me H Me NCOOEt Me H Me NCOOPr Me H Me NCOOiPr Me H Me NCONHEt Me H Me NCONHPr Me H Me NCOH Me H Me NCONHMe Me H Me NCN 138

Me H Me NCOSMe Me H Me NCOSEt Me H Me NCSOMe Me H Me NCSOEt Me H Me NCSOPr Me H Me NSO2H Me H Me NSO2NHMe Me H Me NSO2NMe2 Me H Me NP(O)(OMe)2 Me H Me NP(O)(OEt)2 Me H Me NP(O)Me2 Me H Me NP(O)Et2 Me H Me NP(O)Me(OMe) Me H Me NP(O)(OPr)2 Me H Me NC(O)C(O)H Me H Me NC(O)C(O)Me Me H Me NC(O)C(O)OMe Me H Me NC(O)C(O)OEt Me H Me NC(O)C(O)NH2 Me H Me NC(O)C(O)OH Me H Me NC(NH)H Me H Me NC(NOH)H Me H Me NC(NH)NHMe Me H Me NC(NH)NMe2 Me H Me NC(NH)OMe Me H Me NC(NH)OEt Me Me Me NCOMe Me Me Me NCOEt 139

Me Me Me NCOPr Me Me Me NCHO Me Me Me NCOiPr Me Me Me NCOtBu Me Me Me NCOPh Me Me Me NSO2Me Me Me Me NSO2Et Me Me Me NSO2Pr Me Me Me NSO2Ph Me Me Me NSO2iPr Me Me Me nno2 Me Me Me NCOOMe Me Me Me NCOOEt Me Me Me NCOOPr Me Me Me NCOOiPr Me Me Me NCONHEt Me Me Me NCONHPr Me Me Me NCOH Me Me Me NCONHMe Me Me Me NCN Me Me Me NCOSMe Me Me Me NCOSEt Me Me Me NCSOMe Me Me Me NCSOEt Me Me Me NCSOPr Me Me Me NSO2H Me Me Me NSO2NHMe Me Me Me NSO2NMe2 140

Me Me Me NP(O)(OMe)2 Me Me Me NP(O)(OEt)2 Me Me Me NP(O)Me2 Me Me Me NP(O)Et2 Me Me Me NP(O)Me(OMe) Me Me Me NP(O)(OPr)2 Me Me Me NC(O)C(O)H Me Me Me NC(O)C(O)Me Me Me Me NC(O)C(O)OMe Me Me Me NC(O)C(O)OEt Me Me Me NC(O)C(O)NH2 Me Me Me NC(O)C(O)OH Me Me Me NC(NH)H Me Me Me NC(NOH)H Me Me Me NC(NH)NHMe Me Me Me NC(NH)NMe2 Me Me Me NC(NH)OMe Me Me Me NC(NH)OEt Me Me H NCOMe Me Me H NCOEt Me Me H NCOPr Me Me H NCHO Me Me H NCOiPr Me Me H NCOtBu Me Me H NCOPh Me Me H NSO2Me Me Me H NSO2Et Me Me H NSO2Pr 141

Me Me H NSO,Ph Me Me H NSO2iPr Me Me H nno2 Me Me H NCOOMe Me Me H NCOOEt Me Me H NCOOPr Me Me H NCOOiPr Me Me H NCONHEt Me Me H NCONHPr Me Me H NCOH Me Me H NCONHMe Me Me H NCN Me Me H NCOSMe Me Me H NCOSEt Me Me H NCSOMe Me Me H NCSOEt Me Me H NCSOPr Me Me H nso2h Me Me H NSO2NHMe Me Me H NSO2NMe2 Me Me H NP(O)(OMe)2 Me Me H NP(O)(OEt)2 Me Me H NP(O)Me2 Me Me H NP(O)Et2 Me Me H NP(O)Me(OMe) Me Me H NP(O)(OPr)2 Me Me H NC(O)C(O)H Me Me H NC(O)C(O)Me 142

Me Me H NC(O)C(O)OMe Me Me H NC(O)C(O)OEt Me Me H NC(O)C(O)NH2 Me Me H NC(O)C(O)OH Me Me H NC(NH)H Me Me H NC(NOH)H Me Me H NC(NH)NHMe Me Me H NC(NH)NMe2 Me Me H NC(NH)OMe Me Me H NC(NH)OEt Me CN NH2 NH NH Me CN NHMe NH NH Me CN NMe2 NH NH Me CN NHEt NH NH Et CN NH2 NH NH Et CN NHMe NH NH Et CN NMe2 NH NH Et CN NHEt NH NH cf3 CN NH2 NH NH cf3 CN NHMe NH NH cf3 CN NMe2 NH NH cf3 CN NHEt NH NH 143 TABLE 3

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20 R1 R7 R8 NR2 cf3 CN nh2 NCOMe cf3 CN nh2 NCOEt cf3 CN nh2 NCOPr cf3 CN nh2 NCHO cf3 CN nh2 NCOiPr cf3 CN nh2 NCOtBu cf3 CN nh2 NCOPh cf3 CN nh2 NSO2Me cf3 CN nh2 NSO2Et cf3 CN nh2 NSO2Pr cf3 CN nh2 NSO2Ph cf3 CN nh2 NSO2iPr cf3 CN nh2 nno2

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144 CN NH2 CN NH2 NCOOMe NCOOEt 145 TABLE 3. Continued R1 R7 R8 NR2 cf3 CN nh2 NCOOPr cf3 CN nh2 NCOOiPr cf3 CN nh2 NCONHEt cf3 CN nh2 NCONHPr cf3 CN nh2 nconh2 cf3 CN nh2 NCONHMe cf3 CN nh2 NCN cf3 CN nh2 NCOSMe cf3 CN nh2 NCOSEt cf3 CN nh2 NCSOMe cf3 CN nh2 NCSOEt cf3 CN nh2 NCSOPr cf3 CN nh2 NSO2NH2 cf3 CN nh2 NSO2NHMe cf3 CN nh2 NSO2NMe2 cf3 CN nh2 NP(O)(OMe)2 cf3 CN nh2 NP(O)(OEt)2 cf3 CN nh2 NP(O)Me2 cf3 CN nh2 NP(O)Et2 cf3 CN nh2 NP(O)Me(OMe) cf3 CN nh2 NP(O)(OPr)2 cf3 CN nh2 NC(O)C(O)H cf3 CN nh2 NC(O)C(O)Me cf3 CN nh2 NC(O)C(O)OMe 146 cf3 CN nh2 NC(O)C(O)OEt cf3 CN nh2 NC(O)C(O)NH2 cf3 CN - nh2 NC(O)C(O)OH cf3 CN nh2 NC(NH)NH2 cf3 CN nh2 NC(NOH)NH2 cf3 CN nh2 NC(NH)NHMe cf3 CN nh2 NC(NH)NMe2 cf3 CN nh2 NC(NH)OMe cf3 CN nh2 NC(NH)OEt cf3 CN nh2 NH 0 cf3 CN nh2 NCOMe 0 cf3 CN nh2 NCOEt 0 cf3 CN nh2 NCOPr 0 cf3 CN nh2 NCHO 0 cf3 CN nh2 NCOiPr 0 cf3 CN nh2 NCOtBu 0 cf3 CN nh2 NCOPh 0 cf3 CN nh2 NSO2Me 0 cf3 CN nh2 NSO2Et 0 cf3 CN nh2 NSO2Pr 0 cf3 CN nh2 NSO2Ph 0 cf3 CN nh2 NSO2iPr 0 cf3 CN nh2 nno2 0 cf3 CN nh2 NCOOMe 0 cf3 CN nh2 NCOOEt 0 cf3 CN nh2 NCOOPr 0 cf3 CN nh2 NCOOiPr 0 cf3 CN nh2 NCONHEt 0 147 CF3 CN NH2 NCONHPr 0 cf3 CN nh2 nconh2 0 cf3 CN nh2 NCONHMe 0 cf3 CN nh2 NCN 0 cf3 CN nh2 NCOSMe 0 cf3 CN nh2 NCOSEt 0 cf3 CN nh2 NCSOMe 0 cf3 CN nh2 NCSOEt 0 cf3 CN nh2 NCSOPr 0 cf3 CN nh2 NSO2NH2 0 cf3 CN nh2 NSO2NHMe 0 cf3 CN nh2 NSO2NMe2 0 cf3 CN nh2 NP(O)(OMe)2 0 cf3 CN nh2 NP(O)(OEt)2 0 cf3 CN nh2 NP(O)Me2 o cf3 CN nh2 NP(O)Et2 0 cf3 CN nh2 NP(O)Me(OMe) 0 cf3 CN nh2 NP(O)(OPr)2 0 cf3 CN nh2 NC(O)C(O)H 0 cf3 CN nh2 NC(O)C(O)Me 0 cf3 CN nh2 NC(O)C(O)OMe 0 cf3 CN nh2 NC(O)C(O)OEt 0 cf3 CN nh2 NC(O)C(O)NH2 0 cf3 CN nh2 NC(O)C(O)OH 0 cf3 CN nh2 NC(NH)NH2 0 cf3 CN nh2 NC(NOH)NH2 0 cf3 CN nh2 NC(NH)NHMe 0 cf3 CN nh2 NC(NH)NMe2 0 148 cf3 CN nh2 NC(NH)OMe cf3 CN nh2 NC(NH)OEt cf3 CN H NCOMe cf3 CN H NCOEt cf3 CN H NCOPr cf3 CN H NCHO gf3 CN H NCOiPr cf3 CN H NCOtBu cf3 CN H NCOPh cf3 CN H NSO2Me cf3 CN H NSO2Et cf3 CN H NSO2Pr cf3 CN H NSO2Ph cf3 CN H NSO2iPr cf3 CN H NNO2 cf3 CN H NCOOMe cf3 CN H NCOOEt cf3 CN H NCOOPr cf3 CN H NCOOiPr cf3 CN H NCONHEt cf3 CN H NCONHPr cf3 CN H NCONH2 cf3 CN H NCONHMe cf3 CN H NCN cf3 CN H NCOSMe cf3 CN H NCOSEt cf3 CN H NCSOMe cf3 CN H NCSOEt 149 cf3 CN H NCSOPr cf3 CN H NSO2NH2 cf3 CN H NSO2NHMe cf3 CN H NSO2NMe2 cf3 CN H NP(O)(OMe)2 cf3 CN H NP(O)(OEt)2 cf3 CN H NP(O)Me2 cf3 CN H NP(O)Et2 cf3 CN H NP(O)Me(OMe) cf3 CN H NP(O)(OPr)2 cf3 CN H NC(O)C(O)H cf3 CN H NC(O)C(O)Me cf3 CN H NC(O)C(O)OMe cf3 CN H NC(O)C(O)OEt cf3 CN H NC(O)C(O)NH2 cf3 CN H NC(O)C(O)OH cf3 CN H NC(NH)NH2 cf3 CN H NC(NOH)NH2 cf3 CN H NC(NH)NHMe cf3 CN H NC(NH)NMe2 cf3 CN H NC(NH)OMe cf3 CN H NC(NH)OEt cf3 CN H NH cf3 CN H NCOMe cf3 CN H NCOEt cf3 CN H NCOPr cf3 CN H NCHO cf3 CN H NCOiPr 150 cf3 CN H NCOtBu cf3 CN H NCOPh cf3 cn H NSO2Me cf3 cn H NSO2Et cf3 CN H NSO2Pr cf3 CN H NSO2Ph cf3 CN H NSO2iPr cf3 CN H nno2 cf3 CN H NCOOMe cf3 CN H NCOOEt cf3 CN H NCOOPr cf3 CN H NCOOiPr cf3 CN H NCONHEt cf3 CN H NCONHPr cf3 CN H nconh2 cf3 CN H NCONHMe cf3 CN H NCN cf3 CN H NCOSMe cf3 CN H NCOSEt cf3 CN H NCSOMe cf3 CN H NCSOEt cf3 CN H NCSOPr cf3 CN H NSO2NH2 cf3 CN H NS02NHMe cf3 CN H NSO2NMe2 cf3 CN H NP(0)(0Me)2 cf3 CN H NP(O)(OEt)2 cf3 CN H NP(0)Me2 Ο Ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο 151 cf3 CN H NP(O)Et2 cf3 CN H NP(O)Me(OMe) cf3 CN H NP(O)(OPr)2 cf3 CN H NC(O)C(O)H cf3 CN H NC(O)C(O)Me cf3 CN H NC(O)C(O)OMe cf3 CN H NC(O)C(O)OEt cf3 CN H NC(O)C(O)NH2 cf3 CN H NC(O)C(O)OH cf3 CN H NC(NH)NH2 cf3 CN H NC(NOH)NH2 cf3 CN H NC(NH)NHMe cf3 CN H NC(NH)NMe2 cf3 CN H NC(NH)OMe cf3 CN H NC(NH)OEt cf3 CN SMe NCOMe cf3 CN SMe NCOEt cf3 CN SMe NCOPr cf3 CN SMe NCHO cf3 CN SMe NCOiPr cf3 CN SMe NCOtBu cf3 CN SMe NCOPh cf3 CN SMe NSO2Me cf3 CN SMe NSO2Et cf3 CN SMe NSO2Pr cf3 CN SMe NSO2Ph cf3 CN SMe NSO2iPr cf3 CN SMe NNO2 Ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο 152 CF3 CN SMe NCOOMe cf3 CN SMe NCOOEt cf3 CN SMe NCOOPr cf3 CN SMe NCOOiPr cf3 CN SMe NCONHEt cf3 CN SMe NCONHPr cf3 CN SMe NCONH2 cf3 CN SMe NCONHMe cf3 CN SMe NCN cf3 CN SMe NCOSMe cf3 CN SMe NCOSEt cf3 CN SMe NCSOMe cf3 CN SMe NCSOEt cf3 CN SMe NCSOPr cf3 CN SMe NSO2NH2 cf3 CN SMe NSO2NHMe cf3 CN SMe NSO2NMe2 cf3 CN SMe NP(O)(OMe)2 cf3 CN SMe NP(O)(OEt)2 cf3 CN SMe NP(O)Me2 cf3 CN SMe NP(O)Et2 cf3 CN SMe NP(O)Me(OMe) cf3 CN SMe NP(O)(OPr)2 cf3 CN SMe NC(O)C(O)H cf3 CN SMe NC(O)C(O)Me cf3 CN SMe NC(O)C(O)OMe cf3 CN SMe NC(O)C(O)OEt cf3 CN SMe NC(O)C(O)NH2 153

cf3 CN SMe NC(O)C(O)OH cf3 CN SMe NC(NH)NH2 cf3 CN SMe NC(NOH)NH2 cf3 CN SMe NC(NH)NHMe cf3 CN SMe NC(NH)NMe2 cf3 CN SMe NC(NH)OMe cf3 CN SMe NC(NH)OEt cf3 CN SMe NCOMe 0 cf3 CN SMe NCOEt 0 cf3 CN SMe NCOPr 0 cf3 CN SMe NCHO 0 cf3 CN SMe NCOiPr 0 cf3 CN SMe NCOtBu 0 cf3 CN SMe NCOPh 0 cf3 CN SMe NSO2Me 0 cf3 CN SMe NSO2Et 0 cf3 CN SMe NSO2Pr 0 cf3 CN SMe NSO2Ph 0 cf3 CN SMe NSO2iPr 0 cf3 CN SMe nno2 0 cf3 CN SMe NCOOMe 0 cf3 CN SMe NCOOEt 0 cf3 CN SMe NCOOPr 0 cf3 CN SMe NCOOiPr 0 cf3 CN SMe NCONHEt 0 cf3 CN SMe NCONHPr 0 cf3 CN SMe nconh2 0 cf3 CN SMe NCONHMe O 154 cf3 CN SMe NCN 0 cf3 CN SMe NCOSMe 0 cf3 CN SMe NCOSEt 0 cf3 CN SMe NCSOMe O cf3 CN SMe NCSOEt 0 cf3 CN SMe NCSOPr 0 cf3 CN SMe NSO2NH2 O cf3 CN SMe NS02NHMe O cf3 CN SMe NSO2NMe2 0 cf3 CN SMe NP(O)(OMe)2 0 cf3 CN SMe NP(O)(OEt)2 0 cf3 CN SMe NP(O)Me2 0 cf3 CN SMe NP(O)Et2 0 cf3 CN SMe NP(O)Me(OMe) 0 cf3 CN SMe NP(O)(OPr)2 0 cf3 CN SMe NC(O)C(O)H 0 cf3 CN SMe NC(O)C(O)Me O cf3 CN SMe NC(O)C(O)OMe 0 cf3 CN . SMe NC(O)C(O)OEt 0 cf3 CN SMe NC(O)C(O)NH2 0 cf3 CN SMe NC(O)C(O)OH 0 cf3 CN SMe NC(NH)NH2 0 cf3 CN SMe NC(NOH)NH2 0 cf3 CN SMe NC(NH)NHMe 0 cf3 CN SMe NC(NH)NMe2 0 cf3 CN SMe NC(NH)OMe 0 cf3 CN SMe NC(NH)OEt 0 cf3 CN Cl NCOMe

I 155 cf3 CN Cl NCOEt cf3 CN Cl NCOPr cf3 CN Cl NCHO cf3 CN Cl NCOiPr cf3 CN Cl NCOtBu cf3 CN Cl NCOPh cf3 CN Cl NSO2Me cf3 CN Cl NSO2Et cf3 CN Cl NSO2Pr cf3 CN Cl NSO2Ph cf3 CN Cl NSO2iPr cf3 CN Cl nno2 cf3 CN Cl NCOOMe cf3 CN Cl NCOOEt cf3 CN Cl NCOOPr cf3 CN Cl NCOOiPr cf3 CN Cl NCONHEt cf3 CN Cl NCONHPr cf3 CN Cl NCONH2 cf3 CN Cl NCONHMe cf3 CN Cl NCN cf3 CN Cl NCOSMe cf3 CN Cl NCOSEt cf3 CN Cl NCSOMe cf3 CN Cl NCSOEt cf3 CN Cl NCSOPr cf3 CN Cl NSO2NH2 cf3 CN Cl NSO2NHMe 156

cf3 CN Cl NSO2NMe2 cf3 CN Cl NP(O)(OMe)2 cf3 CN Cl NP(O)(OEt)2 cf3 CN Cl NP(O)Me2 cf3 CN Cl NP(O)Et2 cf3 CN Cl NP(O)Me(OMe) cf3 CN Cl NP(O)(OPr)2 cf3 CN Cl NC(O)C[O)H cf3 CN Cl NC(O)C(O)Me cf3 CN Cl NC(O)C(O)OMe cf3 CN Cl NC(O)C(O)OEt cf3 CN Cl NC(O)C(O)NH2 cf3 CN Cl NC(O)C(O)OH cf3 CN Cl NC(NH)NH2 cf3 CN Cl NC(NOH)NH2 cf3 CN Cl NC(NH)NHMe cf3 CN Cl NC(NH)NMe2 cf3 CN Cl NC(NH)OMe cf3 CN Cl NC(NH)OEt cf3 CN Cl NCOMe 0 cf3 CN Cl NCOEt 0 cf3 CN Cl NCOPr 0 cf3 CN Cl NCHO 0 cf3 CN Cl NCOiPr 0 cf3 CN Cl NCOtBu 0 cf3 CN Cl NCOPh 0 cf3 CN Cl NSO2Me 0 cf3 CN Cl NSO2Et O 157 cf3 CN Cl NSO2Pr 0 cf3 CN Cl NSO2Ph 0 cf3 CN Cl NSO2iPr O cf3 CN Cl nno2 0 cf3 CN Cl NCOOMe 0 cf3 CN Cl NCOOEt 0 cf3 CN Cl NCOOPr 0 cf3 CN Cl NCOOiPr 0 cf3 CN Cl NCONHEt 0 cf3 CN Cl NCONHPr 0 cf3 CN Cl NCONH2 0 cf3 CN Cl NCONHMe 0 cf3 CN Cl NCN 0 cf3 CN Cl NCOSMe 0 CF3 CN Cl NCOSEt 0 cf3 CN Cl NCSOMe 0 cf3 CN Cl NCSOEt 0 cf3 CN Cl NCSOPr 0 cf3 CN Cl NSO2NH2 0 cf3 CN Cl NSO2NHMe 0 cf3 CN Cl NSO2NMe2 O cf3 CN Cl NP(O)(OMe)2 0 cf3 CN Cl NP(O)(OEt)2 0 cf3 CN Cl NP(O)Me2 0 cf3 CN Cl NP(O)Et2 0 cf3 CN Cl NP(O)Me(OMe) O cf3 CN Cl NP(O)(OPr)2 0 cf3 CN Cl NC(O)C(O)H 0 158 cf3 CN Cl NC(O)C(O)Me 0 cf3 CN Cl NC(O)C(O)OMe 0 cf3 CN Cl NC(O)C(O)OEt 0 cf3 CN Cl NC(O)C(O)NH2 0 cf3 CN Cl NC(O)C(O)OH 0 cf3 CN Cl NC(NH)NH2 0 cf3 CN Cl NC(NOH)NH2 0 cf3 CN Cl NC(NH)NHMe 0 cf3 CN Cl NC(NH)NMe2 0 cf3 CN Cl NC(NH)OMe 0 cf3 CN Cl NC(NH)OEt 0

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159 TABLE 4

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R1 R9 R11 NR2 cf3 H H NCOMe cf3 H H NCOEt cf3 H H NCOPr cf3 H H NCHO cf3 H H NCOiPr cf3 H H NCOtBu cf3 H H NCOPh cf3 H H NSO2Me cf3 H H NSO2Et cf3 H H NSO2Pr cf3 H H NSO2Ph cf3 H H NSO2iPr 160 CF3 H H nno2 cf3 H H NCOOMe cf3 H H NCOOEt cf3 H H NCOOPr 161 TABLE 4, Continued R1 R9 R11 NR2 cf3 H H NCOOiPr cf3 H H NCONHEt cf3 H H NCONHPr cf3 H H NCONH2 cf3 H H NCONHMe cf3 H H NCN cf3 H H NCOSMe cf3 H H NCOSEt cf3 H H NCSOMe cf3 H H NCSOEt cf3 H H NCSOPr cf3 H H NSO2NH2 cf3 H H NSO2NHMe cf3 H H NSO2NMe2 cf3 H H NP(O)(OMe)2 cf3 H H NP(O)(OEt)2 cf3 H H NP(O)Me2 cf3 H H NP(O)Et2 cf3 H H NP(O)Me(OMe) cf3 H H NP(O)(OPr)2 cf3 H H NC(O)C(O)H cf3 H H NC(O)C(O)Me cf3 H H NC(O)C(O)OMe cf3 H H NC(O)C(O)OEt 162 cf3 H H NC(O)C(O)NH2 cf3 H H NC(O)C(O)OH cf3 H H NC(NH)NH2 cf3 H H NC(NOH)NH2 cf3 H H NC(NH)NHMe cf3 H H NC(NH)NMe2 cf3 H H NC(NH)OMe cf3 H H NC(NH)OEt cf3 Cl H NCOMe cf3 Cl H NCOEt cf3 Cl H NCOPr cf3 Cl H NCHO cf3 Cl H NCOiPr cf3 Cl H NCOtBu cf3 Cl H NCOPh cf3 Cl H NSO2Me cf3 Cl H NSO2Et cf3 Cl H NSO2Pr cf3 Cl H NSO2Ph cf3 Cl H NSO2iPr cf3 Cl H nno2 cf3 Cl H NCOOMe cf3 Cl H NCOOEt cf3 Cl H NCOOPr cf3 Cl H NCOOiPr cf3 Cl H NCONHEt cf3 Cl H NCONHPr cf3 Cl H NCONH2 163 cf3 Cl H NCONHMe cf3 Cl H NCN cf3 Cl H NCOSMe cf3 Cl H NCOSEt cf3 Cl H NCSOMe cf3 Cl H NCSOEt cf3 Cl H NCSOPr cf3 Cl H NSO2NH2 cf3 Cl H NSO2NHMe cf3 Cl H NSO2NMe2 cf3 Cl H NP(O)(OMe)2 cf3 Cl H NP(O)(OEt)2 cf3 Cl H NP(O)Me2 cf3 Cl H NP(O)Et2 cf3 Cl H NP(O)Me(OMe) cf3 Cl H NP(O)(OPr)2 cf3 Cl H NC(O)C(O)H cf3 Cl H NC(O)C(O)Me cf3 Cl H NC(O)C(O)OMe cf3 Cl H NC(O)C(O)OEt cf3 Cl H NC(O)C(O)NH2 cf3 Cl H NC(O)C(O)OH cf3 Cl H NC(NH)NH2 cf3 Cl H NC(NOH)NH2 cf3 Cl H NC(NH)NHMe cf3 Cl H NC(NH)NMe2 cf3 Cl H NC(NH)OMe cf3 Cl H NC(NH)OEt 164 cf3 Cl Me NCOMe cf3 Cl Me NCOEt cf3 Cl Me NCOPr cf3 Cl Me NCHO cf3 Cl Me NCOiPr cf3 Cl Me NCOtBu cf3 Cl Me NCOPh cf3 Cl Me NSO2Me cf3 Cl Me NSO2Et cf3 Cl Me NSO2Pr cf3 Cl Me NSO2Ph cf3 Cl Me NSO2iPr cf3 Cl Me nno2 cf3 Cl Me NCOOMe cf3 Cl Me NCOOEt cf3 Cl Me NCOOPr cf3 Cl Me NCOOiPr cf3 Cl Me NCONHEt cf3 Cl Me NCONHPr cf3 Cl Me NCONH2 cf3 Cl Me NCONHMe cf3 Cl Me NCN cf3 Cl Me NCOSMe cf3 Cl Me NCOSEt cf3 Cl Me NCSOMe cf3 Cl Me NCSOEt cf3 Cl Me NCSOPr cf3 Cl Me NSO2NH2 165 cf3 Cl Me NSO2NHMe cf3 Cl Me NSO2NMe2 cf3 Cl Me NP(O)(OMe)2 cf3 Cl Me NP(O)(OEt)2 cf3 Cl Me NP(O)Me2 cf3 Cl Me NP(O)Et2 cf3 Cl Me NP(O)Me(OMe) cf3 Cl Me NP(O)(OPr)2 cf3 Cl Me NC(O)C(O)H cf3 Cl Me NC(O)C(O)Me cf3 Cl Me NC(O)C(O)OMe cf3 Cl Me NC(O)C(O)OEt cf3 Cl Me NC(O)C(O)NH2 cf3 Cl Me NC(O)C(O)OH cf3 Cl Me NC(NH)NH2 cf3 Cl Me NC(NOH)NH2 cf3 Cl Me NC(NH)NHMe cf3 Cl Me NC(NH)NMe2 cf3 Cl Me NC(NH)OMe cf3 Cl Me NC(NH)OEt cf3 Cl SMe NCOMe cf3 Cl SMe NCOEt cf3 Cl SMe NCOPr cf3 Cl SMe NCHO cf3 Cl SMe NCOiPr cf3 Cl SMe NCOtBu cf3 Cl SMe NCOPh cf3 Cl SMe NSO2Me 166 cf3 Cl SMe NSO2Et cf3 Cl SMe NSO2Pr cf3 Cl SMe NSO2Ph cf3 Cl SMe NSO2iPr cf3 Cl SMe nno2 cf3 Cl SMe NCOOMe cf3 Cl SMe NCOOEt cf3 Cl SMe NCOOPr cf3 Cl SMe NCOOiPr cf3 Cl SMe NCONHEt cf3 Cl SMe NCONHPr cf3 Cl SMe nconh2 cf3 Cl SMe NCONHMe cf3 Cl SMe NCN cf3 Cl SMe NCOSMe cf3 Cl SMe NCOSEt cf3 Cl SMe NCSOMe cf3 Cl SMe NCSOEt cf3 Cl SMe NCSOPr cf3 Cl SMe NSO2NH2 cf3 Cl SMe NSO2NHMe cf3 Cl SMe NSO2NMe2 cf3 Cl SMe NP(O)(OMe)2 cf3 Cl SMe NP(O)(OEt)2 cf3 Cl SMe NP(O)Me2 cf3 Cl SMe NP(O)Et2 cf3 Cl SMe NP(O)Me(OMe) cf3 Cl SMe NP(O)(OPr)2 167 CF3 Cl SMe NC(O)C(O)H cf3 Cl SMe NC(O)C(O)Me cf3 Cl SMe NC(O)C(O)OMe cf3 Cl SMe NC(O)C(O)OEt cf3 Cl SMe NC(O)C(O)NH2 cf3 Cl SMe NC(O)C(O)OH cf3 Cl SMe NC(NH)NH2 cf3 Cl SMe NC(NOH)NH2 cf3 Cl SMe NC(NH)NHMe cf3 Cl SMe NC(NH)NMe2 cf3 Cl SMe NC(NH)OMe cf3 Cl SMe NC(NH)OEt cf3 H Me NCOMe cf3 H Me NCOEt cf3 H Me NCOPr cf3 H Me NCHO cf3 H Me NCOiPr cf3 H Me NCOtBu cf3 H Me NCOPh cf3 H Me NSO2Me cf3 H Me NSO2Et cf3 H Me NSO2Pr cf3 H Me NSO2Ph cf3 H Me NSO2iPr cf3 H Me nno2 cf3 H Me NCOOMe cf3 H Me NCOOEt cf3 H Me NCOOPr 168 cf3 H Me NCOOiPr cf3 H Me NCONHEt cf3 H Me NCONHPr cf3 H Me NCONH2 cf3 H Me NCONHMe cf3 H Me NCN cf3 H Me NCOSMe cf3 H Me NCOSEt cf3 H Me NCSOMe cf3 H Me NCSOEt cf3 H Me NCSOPr cf3 H Me NSO2NH2 cf3 H Me NSO2NHMe cf3 H Me NSO2NMe2 cf3 H Me NP(O)(OMe)2 cf3 H Me NP(O)(OEt)2 cf3 H Me NP(O)Me2 cf3 H Me NP(O)Et2 cf3 H Me NP(O)Me(OMe) cf3 H Me NP(O)(OPr)2 cf3 H Me NC(O)C(O)H cf3 H Me NC(O)C(O)Me cf3 H Me NC(O)C(O)OMe cf3 H Me NC(O)C(O)OEt cf3 H Me NC(O)C(O)NH2 cf3 H Me NC(O)C(O)OH cf3 H Me NC(NH)NH2 cf3 H Me NC(NOH)NH2 169 CF3 H Me NC(NH)NHMe cf3 H Me NC(NH)NMe2 cf3 H Me NC(NH)OMe cf3 H Me NC(NH)OEt cf3 H SMe NCOMe cf3 H SMe NCOEt cf3 H SMe NCOPr cf3 H SMe NCHO cf3 H SMe NCOiPr cf3 H SMe NCOtBu cf3 H SMe NCOPh cf3 H SMe NSO2Me cf3 H SMe NSO2Et cf3 H SMe NSO2Pr cf3 H SMe NSO2Ph cf3 H SMe NSO2iPr cf3 H SMe nno2 cf3 H SMe NCOOMe cf3 H SMe NCOOEt cf3 H SMe NCOOPr cf3 H SMe NCOOiPr cf3 H SMe NCONHEt cf3 H SMe NCONHPr cf3 H SMe NCONH2 cf3 H SMe NCONHMe cf3 ! H SMe NCN cf3 H SMe NCOSMe cf3 H SMe NCOSEt 170

cf3 H SMe NCSOMe cf3 H SMe NCSOEt cf3 H SMe NCSOPr cf3 H SMe NSO2NH2 cf3 H SMe NS02NHMe cf3 H SMe NSO2NMe2 cf3 H SMe NP(O)(OMe)2 cf3 H SMe NP(O)(OEt)2 cf3 H SMe NP(O)Me2 cf3 H SMe NP(O)Et2 cf3 H SMe NP(O)Me(OMe) cf3 H SMe NP(O)(OPr)2 cf3 H SMe NC(O)C(O)H cf3 H SMe NC(O)C(O)Me cf3 H SMe NC(0)C(0)0Me cf3 H SMe NC(O)C(O)OEt cf3 H SMe NC(O)C(O)NH2 cf3 H SMe NC(O)C(O)OH cf3 H SMe NC(NH)NH2 cf3 H SMe NC(N0H)NH2 cf3 H SMe NC(NH)NHMe cf3 H SMe NC(NH)NMe2 cf3 H SMe NC(NH)0Me cf3 H SMe NC(NH)OEt cf3 Me H NCOMe cf3 Me H NCOEt cf3 Me H NCOPr cf3 Me H NCHO 171 cf3 Me H NCOiPr cf3 Me H NCOtBu cf3 Me H NCOPh cf3 Me H NSO2Me cf3 Me H NSO2Et cf3 Me H NSO2Pr cf3 Me H NSO2Ph cf3 Me H NSO2iPr cf3 Me H nno2 cf3 Me H NCOOMe cf3 Me H NCOOEt cf3 Me H NCOOPr cf3 Me H NCOOiPr cf3 Me H NCONHEt cf3 Me H NCONHPr cf3 Me H nconh2 cf3 Me H NCONHMe cf3 Me H NCN cf3 Me H NCOSMe cf3 Me H NCOSEt cf3 Me H NCSOMe cf3 Me H NCSOEt cf3 Me H NCSOPr cf3 Me H nso2nh2 cf3 Me H NSO2NHMe cf3 Me H NSO2NMe2 cf3 Me H NP(O)(OMe)2 cf3 Me H NP(O)(OEt)2 172 cf3 Me H NP(O)Me2 cf3 Me H NP(O)Et2 cf3 Me H NP(O)Me(OMe) cf3 Me H NP(O)(OPr)2 cf3 Me H NC(O)C(O)H cf3 Me H NC(O)C(O)Me cf3 Me H NC(0)C(0)OMe cf3 Me H NC(O)C(O)OEt cf3 Me H NC(O)C(O)NH2 cf3 Me H NC(O)C(O)OH cf3 Me H NC(NH)NH2 cf3 Me H NC(NOH)NH2 cf3 Me H NC(NH)NHMe cf3 Me H NC(NH)NMe2 cf3 Me H NC(NH)OMe cf3 Me H NC(NH)OEt cf3 Me Me NCOMe cf3 Me Me NCOEt cf3 Me Me NCOPr cf3 Me Me NCHO cf3 Me Me NCOiPr cf3 Me Me NCOtBu cf3 Me Me NCOPh cf3 Me Me NSO2Me cf3 Me Me NSO2Et cf3 Me Me NSO2Pr cf3 Me Me NSO2Ph cf3 Me Me NSO2iPr 173 cf3 Me Me nno2 cf3 Me Me NCOOMe cf3 Me Me NCOOEt cf3 Me Me NCOOPr cf3 Me Me NCOOiPr cf3 Me Me NCONHEt cf3 Me Me NCONHPr cf3 Me Me NCONH2 cf3 Me Me NCONHMe cf3 Me Me NCN cf3 Me Me NCOSMe cf3 Me Me NCOSEt cf3 Me Me NCSOMe cf3 Me Me NCSOEt cf3 Me Me NCSOPr cf3 Me Me NSO2NH2 cf3 Me Me NSO2NHMe cf3 Me Me NSO2NMe2 cf3 Me Me NP(O)(OMe)2 cf3 Me Me NP(O)(OEt)2 cf3 Me Me NP(O)Me2 cf3 Me Me NP(O)Et2 cf3 Me Me NP(O)Me(OMe) cf3 Me Me NP(O)(OPr)2 cf3 Me Me NC(O)C(O)H cf3 Me Me NC(O)C(O)Me cf3 Me Me NC(O)C(O)OMe cf3 Me Me NC(O)C(O)OEt 174 cf3 Me Me NC(O)C(O)NH2 cf3 Me Me NC(O)C(O)OH cf3 Me Me NC(NH)NH2 cf3 Me Me NC(NOH)NH2 cf3 Me Me NC(NH)NHMe cf3 Me Me NC(NH)NMe2 cf3 Me Me NC(NH)OMe cf3 Me Me NC(NH)OEt Me H H NCOMe Me H H NCOEt Me H H NCOPr Me H H NCHO Me H H NCOiPr Me H H NCOtBu Me H H NCOPh Me H H NSO2Me Me H H NSO2Et Me H H NSO2Pr Me H H NSO2Ph Me H H NSO2iPr Me H H nno2 Me H H NCOOMe Me H H NCOOEt Me H H NCOOPr Me H H NCOOiPr Me H H NCONHEt Me H H NCONHPr Me H H NCONH2 175

Me H H NCONHMe Me H H NCN Me H H NCOSMe Me H H NCOSEt Me H H NCSOMe Me H H NCSOEt Me H H NCSOPr Me H H NSO2NH2 Me H H NSO2NHMe Me H H NSO2NMe2 Me H H NP(O)(OMe)2 Me H H NP(O)(OEt)2 Me H H NP(O)Me2 Me H H NP(O)Et2 Me H H NP(O)Me(OMe) Me H H NP(O)(OPr)2 Me H H NC(O)C(O)H Me H H NC(O)C(O)Me Me H H NC(O)C(O)OMe Me H H NC(O)C(O)OEt Me H H NC(O)C(O)NH2 Me H H NC(O)C(O)OH Me H H NC(NH)NH2 Me H H NC(NOH)NH2 Me H H NC(NH)NHMe Me H H NC(NH)NMe2 Me H H NC(NH)OMe Me H H NC(NH)OEt 176

Me Cl H NCOMe Me Cl H NCOEt Me Cl H NCOPr Me Cl H NCHO Me Cl H NCOiPr Me Cl H NCOtBu Me Cl H NCOPh Me Cl H NSO2Me Me Cl H NSO2Et Me Cl H NSO2Pr Me Cl H NSO2Ph Me Cl H NSO2iPr Me Cl H NNO2 Me Cl H NCOOMe Me Cl H NCOOEt Me Cl H NCOOPr Me Cl H NCOOiPr Me Cl H NCONHEt Me Cl H NCONHPr Me Cl H NCONH2 Me Cl H NCONHMe Me Cl H NCN Me Cl H NCOSMe Me Cl H NCOSEt Me Cl H NCSOMe Me Cl H NCSOEt Me Cl H NCSOPr Me Cl H NSO2NH2 177

Me Cl H NSO,NHMe Me Cl H NSO2NMe2 Me Cl H NP(O)(OMe)2 Me Cl H NP(O)(OEt)2 Me Cl H NP(O)Me2 Me Cl H NP(O)Et2 Me Cl H NP(O)Me(OMe) Me Cl H NP(O)(OPr)2 Me Cl H NC(O)C(O)H Me Cl H NC(O)C(O)Me Me Cl H NC(O)C(O)OMe Me Cl H NC(O)C(O)OEt Me Cl H NC(O)C(O)NH2 Me Cl H NC(O)C(O)OH Me Cl H NC(NH)NH2 Me Cl H NC(NOH)NH2 Me Cl H NC(NH)NHMe Me Cl H NC(NH)NMe2 Me Cl H NC(NH)OMe Me Cl H NC(NH)OEt Me Cl Me NCOMe Me Cl Me NCOEt Me Cl Me NCOPr Me Cl Me NCHO Me Cl Me NCOiPr Me Cl Me NCOtBu Me Cl Me NCOPh Me Cl Me NSO2Me

Me

Cl H INCdNHIlNlVXe? 178

Me Cl Me NSO2Et Me Cl Me NSO2Pr Me Cl Me NSO2Ph Me Cl Me NSO2iPr Me Cl Me nno2 Me Cl Me NCOOMe Me Cl Me NCOOEt Me Cl Me NCOOPr Me Cl Me NCOOiPr Me Cl Me NCONHEt Me Cl Me NCONHPr Me Cl Me NCONH2 Me Cl Me NCONHMe Me Cl Me NCN Me Cl Me NCOSMe Me Cl Me NCOSEt Me Cl Me NCSOMe Me Cl Me NCSOEt Me Cl Me NCSOPr Me Cl Me NSO2NH2 Me Cl Me NSO2NHMe Me Cl Me NSO2NMe2 Me Cl Me NP(O)(OMe)2 Me Cl Me NP(O)(OEt)2 Me Cl Me NP(O)Me2 Me Cl Me NP(O)Et2 Me Cl Me NP(O)Me(OMe) Me Cl Me NP(O)(OPr)2 179

Me Cl Me NC(O)C(O)H Me Cl Me NC(O)C(O)Me Me Cl Me NC(O)C(O)OMe Me Cl Me NC(O)C(O)OEt Me Cl Me NC(O)C(O)NH2 Me Cl Me NC(O)C(O)OH Me Cl Me NC(NH)NH2 Me Cl Me NC(NOH)NH2 Me Cl Me NC(NH)NHMe Me Cl Me NC(NH)NMe2 Me Cl Me NC(NH)OMe Me Cl Me NC(NH)OEt Me Cl SMe NCOMe Me Cl SMe NCOEt Me Cl SMe NCOPr Me Cl SMe NCHO Me Cl SMe NCOiPr Me Cl SMe NCOtBu Me Cl SMe NCOPh Me Cl SMe NSO2Me Me Cl SMe NSO2Et Me Cl SMe NSO2Pr Me Cl SMe NSO2Ph Me Cl SMe NSO2iPr Me Cl SMe NNO2 Me Cl SMe NCOOMe Me Cl SMe NCOOEt Me Cl SMe NCOOPr 180

Me Cl SMe NCOOiPr Me Cl SMe NCONHEt Me Cl SMe NCONHPr Me Cl SMe NCONH2 Me Cl SMe NCONHMe Me Cl SMe NCN Me Cl SMe NCOSMe Me Cl SMe NCOSEt Me Cl SMe NCSOMe Me Cl SMe NCSOEt Me Cl SMe NCSOPr Me Cl SMe NSO2NH2 Me Cl SMe NSO2NHMe Me Cl SMe NSO2NMe2 Me Cl SMe NP(O)(OMe)2 Me Cl SMe NP(O)(OEt)2 Me Cl SMe NP(O)Me2 Me Cl SMe NP(O)Et2 Me Cl SMe NP(O)Me(OMe) Me Cl SMe NP(O)(OPr)2 Me Cl SMe NC(O)C(O)H Me Cl SMe NC(O)C(O)Me Me Cl SMe NC(O)C(O)OMe Me Cl SMe NC(O)C(O)OEt Me Cl SMe NC(O)C(O)NH2 Me Cl SMe NC(O)C(O)OH Me Cl SMe NC(NH)NH2 Me Cl SMe NC(NOH)NH2 181

Me Cl SMe NC(NH)NHMe Me Cl SMe NC(NH)NMe2 Me Cl SMe NC(NH)OMe Me Cl SMe NC(NH)OEt Me H Me NCOMe Me H Me NCOEt Me H Me NCOPr Me H Me NCHO Me H Me NCOiPr Me H Me NCOtBu Me H Me NCOPh Me H Me NSO2Me Me H Me NSO2Et Me H Me NSO2Pr Me H Me NSO2Ph Me H Me NSO2iPr Me H Me NNO2 Me H Me NCOOMe Me H Me NCOOEt Me H Me NCOOPr Me H Me NCOOiPr Me H Me NCONHEt Me H Me NCONHPr Me H Me NCONH2 Me H Me NCONHMe Me H Me NCN Me H Me NCOSMe Me H Me NCOSEt 182

Me H Me NCSOMe Me H Me NCSOEt Me H Me NCSOPr Me H Me NSO2NH2 Me H Me NSO2NHMe Me H Me NSO2NMe2 Me H Me NP(O)(OMe)2 Me H Me NP(O)(OEt)2 Me H Me NP(O)Me2 Me H Me NP(O)Et2 Me H Me NP(O)Me(OMe) Me H Me NP(O)(OPr)2 Me H Me NC(O)C(O)H Me H Me NC(O)C(O)Me Me H Me NC(O)C(O)OMe Me H Me NC(O)C(O)OEt Me H Me NC(O)C(O)NH2 Me H Me NC(O)C(O)OH Me H Me NC(NH)NH2 Me H Me NC(NOH)NH2 Me H Me NC(NH)NHMe Me H Me NC(NH)NMe2 Me H Me NC(NH)OMe Me H Me NC(NH)OEt Me H SMe NCOMe Me H SMe NCOEt Me H SMe NCOPr Me H SMe NCHO 183

Me H SMe NCOiPr Me H SMe NCOtBu Me H SMe NCOPh Me H SMe NSO2Me Me H SMe NSO2Et Me H SMe NSO2Pr Me H SMe NSO2Ph Me H SMe NSO2iPr Me H SMe NNO2 Me H SMe NCOOMe Me H SMe NCOOEt Me H SMe NCOOPr Me H SMe NCOOiPr Me H SMe NCONHEt Me H SMe NCONHPr Me H SMe nconh2 Me H SMe NCONHMe Me H SMe NCN Me H SMe NCOSMe Me H SMe NCOSEt Me H SMe NCSOMe Me H SMe NCSOEt Me H SMe NCSOPr Me H SMe NSO2NH2 Me H SMe NSO2NHMe Me H SMe NSO2NMe2 Me H SMe NP(O)(OMe)2 Me H SMe NP(O)(OEt)2 184

Me H SMe NP(O)Me2 Me H SMe NP(O)Et2 Me H SMe NP(O)Me(OMe) Me H SMe NP(O)(OPr)2 Me H SMe NC(O)C(O)H Me H SMe NC(O)C(O)Me Me H SMe NC(O)C(O)OMe Me H SMe NC(O)C(O)OEt Me H SMe NC(O)C(O)NH2 Me H SMe NC(O)C(O)OH Me H SMe NC(NH)NH2 Me H SMe NC(NOH)NH2 Me H SMe NC(NH)NHMe Me H SMe NC(NH)NMe2 Me H SMe NC(NH)OMe Me H SMe NC(NH)OEt Me Me H NCOMe Me Me H NCOEt Me Me H NCOPr Me Me H NCHO Me Me H NCOiPr Me Me H NCOtBu Me Me H NCOPh Me Me H NSO2Me Me Me H NSO2Et Me Me H NSO2Pr Me Me H NSO2Ph Me Me H NSO2iPr 185

Me Me H nno2 Me Me H NCOOMe Me Me H NCOOEt Me Me H NCOOPr Me Me H NCOOiPr Me Me H NCONHEt Me Me H NCONHPr Me Me H nconh2 Me Me H NCONHMe Me Me H NCN Me Me H NCOSMe Me Me H NCOSEt Me Me H NCSOMe Me Me H NCSOEt Me Me H NCSOPr Me Me H NSO2NH2 Me Me H NSO2NHMe Me Me H NSO2NMe2 Me Me H NP(O)(OMe)2 Me Me H NP(O)(OEt)2 Me Me H NP(O)Me2 Me Me H NP(O)Et2 Me Me H NP(O)Me(OMe) Me Me H NP(O)(OPr)2 Me Me H NC(O)C(O)H Me Me H NC(O)C(O)Me Me Me H NC(O)C(O)OMe Me Me H NC(O)C(O)OEt 186

Me Me H NC(O)C(O)NH2 Me Me H NC(O)C(O)OH Me Me H NC(NH)NH2 Me Me H NC(NOH)NH2 Me Me H NC(NH)NHMe Me Me H NC(NH)NMe2 Me Me H NC(NH)OMe Me Me H NC(NH)OEt Me Me Me NCOMe Me Me Me NCOEt Me Me Me NCOPr Me Me Me NCHO Me Me Me NCOiPr Me Me Me NCOtBu Me Me Me NCOPh Me Me Me NSO2Me Me Me Me NSO2Et Me Me Me NSO2Pr Me Me Me NSO2Ph Me Me Me NSO2iPr Me Me Me nno2 Me Me Me NCOOMe Me Me Me NCOOEt Me Me Me NCOOPr Me Me Me NCOOiPr Me Me Me NCONHEt Me Me Me NCONHPr Me Me Me nconh2 187

Me Me Me NCONHMe Me Me Me NCN Me Me Me NCOSMe Me Me Me NCOSEt Me Me Me NCSOMe Me Me Me NCSOEt Me Me Me NCSOPr Me Me Me NSO2NH2 Me Me Me NSO2NHMe Me Me Me NSO2NMe2 Me Me Me NP(O)(OMe)2 Me Me Me NP(O)(OEt)2 Me Me Me NP(O)Me2 Me Me Me NP(O)Et2 Me Me Me NP(O)Me(OMe) Me Me Me NP(O)(OPr)2 Me Me Me NC(O)C(O)H Me Me Me NC(O)C(O)Me Me Me Me NC(O)C(O)OMe Me Me Me NC(O)C(O)OEt Me Me Me NC(O)C(O)NH2 Me Me Me NC(O)C(O)OH Me Me Me NC(NH)NH2 Me Me Me NC(NOH)NH2 Me Me Me NC(NH)NHMe Me Me Me NC(NH)NMe2 Me Me Me NC(NH)OMe Me Me Me NC(NH)OEt

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188 TABLE 5 10 15 20

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R1 R12 r13 NR2 cf3 Cl Me NCOMe cf3 Cl Me NCOEt cf3 Cl Me NCOPr cf3 Cl Me NCHO cf3 Cl Me NCOiPr cf3 Cl Me NCOtBu cf3 Cl Me NCOPh cf3 Cl Me NSO2Me cf3 Cl Me NSO2Et cf3 Cl Me NSO2Pr cf3 Cl Me NSO2Ph cf3 Cl Me NSO2iPr cf3 Cl Me NNO2

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189 cf3 Cl Me NCOOMe cf3 Cl Me NCOOEt cf3 Cl Me NCOOPr cf3 Cl Me NCOOiPr 190 TABLE 5, Continued R1 R12 R13 NR2 cf3 Cl Me NCONHEt cf3 Cl Me NCONHPr cf3 Cl Me NCONH2 cf3 Cl Me NCONHMe cf3 Cl Me NCN cf3 Cl Me NCOSMe cf3 Cl Me NCOSEt cf3 Cl Me NCSOMe cf3 Cl Me NCSOEt cf3 Cl Me NCSOPr cf3 Cl Me NSO2NH2 cf3 Cl Me NSO2NHMe cf3 Cl Me NSO2NMe2 cf3 Cl Me NP(O)(OMe)2 cf3 Cl Me NP(O)(OEt)2 cf3 Cl Me NP(O)Me2 cf3 Cl Me NP(O)Et2 cf3 Cl Me NP(O)Me(OMe) cf3 Cl Me NP(O)(OPr)2 cf3 Cl Me NC(O)C(O)H cf3 Cl Me NC(O)C(O)Me cf3 Cl Me NC(O)C(O)OMe cf3 Cl Me NC(O)C(O)OEt cf3 Cl Me NC(O)C(O)NH2 191 cf3 Cl Me NC(O)C(O)OH cf3 Cl Me NC(NH)NH2 cf3 Cl Me NC(NOH)NH2 cf3 Cl Me NC(NH)NHMe cf3 Cl Me NC(NH)NMe2 cf3 Cl Me NC(NH)OMe cf3 Cl Me NC(NH)OEt cf3 Cl Me NCOMe 0 cf3 Cl Me NCOEt 0 cf3 Cl Me NCOPr 0 cf3 Cl Me NCHO 0 cf3 Cl Me NCOiPr 0 cf3 Cl Me NCOtBu 0 cf3 Cl Me NCOPh 0 cf3 Cl Me NSO2Me 0 cf3 Cl Me NSO2Et 0 cf3 Cl Me NSO2Pr 0 cf3 Cl Me NSO2Ph 0 cf3 Cl Me NSO2iPr 0 cf3 Cl Me NNO2 0 cf3 Cl Me NCOOMe 0 cf3 Cl Me NCOOEt 0 cf3 Cl Me NCOOPr 0 cf3 Cl Me NCOOiPr 0 cf3 Cl Me NCONHEt 0 cf3 Cl Me NCONHPr 0 cf3 Cl Me NCONH2 0 cf3 Cl Me NCONHMe 0 192 CF3 Cl Me NCN cf3 Cl Me NCOSMe cf3 Cl Me NCOSEt cf3 Cl Me NCSOMe cf3 Cl Me NCSOEt cf3 Cl Me NCSOPr cf3 Cl Me NSO2NH2 cf3 Cl Me NSO2NHMe cf3 Cl Me NSO2NMe2 cf3 Cl Me NP(O)(OMe)2 cf3 Cl Me NP(O)(OEt)2 cf3 Cl Me NP(O)Me2 cf3 Cl Me NP(O)Et2 cf3 Cl Me NP(O)Me(OMe) cf3 Cl Me NP(O)(OPr)2 cf3 Cl Me NC(O)C(O)H cf3 Cl Me NC(O)C(O)Me cf3 Cl Me NC(O)C(O)OMe cf3 Cl Me NC(O)C(O)OEt cf3 Cl Me NC(O)C(O)NH2 cf3 Cl Me NC(O)C(O)OH cf3 Cl Me NC(NH)NH2 cf3 Cl Me NC(NOH)NH2 cf3 Cl Me NC(NH)NHMe cf3 Cl Me NC(NH)NMe2 cf3 Cl Me NC(NH)OMe cf3 Cl Me NC(NH)OEt cf3 H Me NCOMe Ο Ο Ο Ο Ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο 193 cf3 H Me NCOEt cf3 H Me NCOPr cf3 H Me NCHO cf3 H Me NCOiPr cf3 H Me NCOtBu cf3 H Me NCOPh cf3 H Me NSO2Me cf3 H Me NSO2Et cf3 H Me NSO2Pr cf3 H Me NSO2Ph cf3 H Me NSO2iPr cf3 H Me NNO2 cf3 H Me NCOOMe cf3 H Me NCOOEt cf3 H Me NCOOPr cf3 H Me NCOOiPr cf3 H Me NCONHEt cf3 H Me NCONHPr cf3 H Me NCONH2 cf3 H Me NCONHMe cf3 H Me NCN cf3 H Me NCOSMe cf3 H Me NCOSEt cf3 H Me NCSOMe cf3 H Me NCSOEt cf3 H Me NCSOPr cf3 H Me NSO2NH2 cf3 H Me NSO2NHMe 194 CF3 H Me NSO2NMe2 cf3 H Me NP(O)(OMe)2 cf3 H Me NP(O)(OEt)2 cf3 H Me NP(O)Me2 cf3 H Me NP(O)Et2 cf3 H Me NP(O)Me(OMe) cf3 H Me NP(O)(OPr)2 cf3 H Me NC(O)C(O)H cf3 H Me NC(O)C(O)Me cf3 H Me NC(O)C(O)OMe cf3 H Me NC(O)C(O)OEt cf3 H Me NC(O)C(O)NH2 cf3 H Me NC(O)C(O)OH cf3 H Me NC(NH)NH2 cf3 H Me NC(NOH)NH2 cf3 H Me NC(NH)NHMe cf3 H Me NC(NH)NMe2 cf3 H Me NC(NH)OMe cf3 H Me NC(NH)OEt cf3 H Me NCOMe 0 cf3 H Me NCOEt 0 cf3 H Me NCOPr 0 cf3 H Me NCHO 0 cf3 H Me NCOiPr 0 cf3 H Me NCOtBu 0 cf3 H Me NCOPh 0 cf3 H Me NSO2Me 0 cf3 H Me NSO2Et 0 195

cf3 H Me NSOiPr cf3 H Me NSO2Ph cf3 H Me NSO2iPr cf3 H Me nno2 cf3 H Me NCOOMe cf3 H Me NCOOEt cf3 H Me NCOOPr cf3 H Me NCOOiPr cf3 H Me NCONHEt cf3 H Me NCONHPr cf3 H Me nconh2 cf3 H Me NCONHMe cf3 H Me NCN cf3 H Me NCOSMe cf3 H Me NCOSEt cf3 H Me NCSOMe cf3 H Me NCSOEt cf3 H Me NCSOPr cf3 H Me nso2nh2 cf3 H Me NSO2NHMe cf3 H Me NSO2NMe2 cf3 H Me NP(O)(OMe)2 cf3 H Me NP(O)(OEt)2 cf3 H Me NP(O)Me2 cf3 H Me NP(O)Et2 cf3 H Me NP(O)Me(OMe) cf3 H Me NP(O)(OPr)2 cf3 H Me NC(O)C(O)H Ο Ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο ο 196 CF3 H Me NC(O)C(O)Me 0 cf3 H Me NC(O)C(O)OMe 0 cf3 H Me NC(O)C(O)OEt 0 cf3 H Me NC(O)C(O)NH2 0 cf3 H Me NC(O)C(O)OH 0 cf3 H Me NC(NH)NH2 0 cf3 H Me NC(NOH)NH2 0 cf3 H Me NC(NH)NHMe 0 cf3 H Me NC(NH)NMe2 0 cf3 H Me NC(NH)OMe 0 cf3 H Me NC(NH)OEt 0 cf3 Me Me NCOMe cf3 Me Me NCOEt cf3 Me Me NCOPr cf3 Me Me NCHO cf3 Me Me NCOiPr cf3 Me Me NCOtBu cf3 Me Me NCOPh cf3 Me Me NSO2Me cf3 Me Me NSO2Et cf3 Me Me NSO2Pr cf3 Me Me NSO2Ph cf3 Me Me NSO2iPr cf3 Me Me nno2 cf3 Me Me NCOOMe cf3 Me Me NCOOEt cf3 Me Me NCOOPr cf3 Me Me NCOOiPr 197 cf3 Me Me NCONHEt cf3 Me Me NCONHPr cf3 Me Me NCONH2 cf3 Me Me NCONHMe cf3 Me Me NCN cf3 Me Me NCOSMe cf3 Me Me NCOSEt cf3 Me Me NCSOMe cf3 Me Me NCSOEt cf3 Me Me NCSOPr cf3 Me Me NSO2NH2 cf3 Me Me NSO2NHMe cf3 Me Me NSO2NMe2 cf3 Me Me NP(O)(OMe)2 cf3 Me Me NP(O)(OEt)2 cf3 Me Me NP(O)Me2 cf3 Me Me NP(O)Et2 cf3 Me Me NP(O)Me(OMe) cf3 Me Me NP(O)(OPiQ2 cf3 Me Me NC(O)C(O)H cf3 Me Me NC(O)C(O)Me cf3 Me Me NC(O)C(O)OMe cf3 Me Me NC(O)C(O)OEt cf3 Me Me NC(O)C(O)NH2 cf3 Me Me NC(O)C(O)OH cf3 Me Me NC(NH)NH2 cf3 Me Me NC(NOH)NH2 cf3 Me Me NC(NH)NHMe 198 cf3 Me Me NC(NH)NMe2 cf3 Me Me NC(NH)OMe cf3 Me Me NC(NH)OEt cf3 Me Me NCOMe 0 cf3 Me Me NCOEt O cf3 Me Me NCOPr 0 cf3 Me Me NCHO O cf3 Me Me NCOiPr 0 cf3 Me Me NCOtBu 0 cf3 Me Me NCOPh O cf3 Me Me NSO2Me O cf3 Me Me NSO2Et O cf3 Me Me NSO2Pr O cf3 Me Me NSO2Ph 0 cf3 Me Me NSO2iPr O cf3 Me Me nno2 0 cf3 Me Me NCOOMe 0 cf3 Me Me NCOOEt 0 cf3 Me Me NCOOPr 0 cf3 Me Me NCOOiPr O cf3 Me Me NCONHEt 0 cf3 Me Me NCONHPr 0 cf3 Me Me NCONH2 0 cf3 Me Me NCONHMe 0 cf3 Me Me NCN 0 cf3 Me Me NCOSMe 0 cf3 Me Me NCOSEt 0 cf3 Me Me NCSOMe 0 199 cf3 Me Me NCSOEt O cf3 Me Me NCSOPr O cf3 Me Me NSO2NH2 0 cf3 Me Me NSO2NHMe 0 cf3 Me Me NSO2NMe2 0 cf3 Me Me NP(O)(OMe)2 0 cf3 Me Me NP(O)(OEt)2 0 cf3 Me Me NP(O)Me2 0 cf3 Me Me NP(O)Et2 0 cf3 Me Me NP(O)Me(OMe) 0 cf3 Me Me NP(O)(OPr)2 0 cf3 Me Me NC(O)C(O)H 0 cf3 Me Me NC(O)C(O)Me O cf3 Me Me NC(O)C(O)OMe 0 cf3 Me Me NC(O)C(O)OEt 0 cf3 Me Me NC(O)C(O)NH2 0 cf3 Me Me NC(O)C(O)OH O cf3 Me Me NC(NH)NH2 O cf3 Me Me NC(NOH)NH2 0 cf3 Me Me NC(NH)NHMe 0 cf3 Me Me NC(NH)NMe2 0 cf3 Me Me NC(NH)OMe 0 cf3 Me Me NC(NH)OEt 0 cf3 Cl Cl NCOMe cf3 Cl Cl NCOEt cf3 Cl Cl NCOPr cf3 Cl Cl NCHO cf3 Cl Cl NCOiPr 200 cf3 Cl Cl NCOtBu cf3 Cl Cl NCOPh cf3 Cl Cl NSO2Me cf3 Cl Cl NSO2Et cf3 Cl Cl NSO2Pr cf3 Cl Cl NSO2Ph cf3 Cl Cl NSO2iPr cf3 Cl Cl nno2 cf3 Cl Cl NCOOMe cf3 Cl Cl NCOOEt cf3 Cl Cl NCOOPr cf3 Cl Cl NCOOiPr cf3 Cl Cl NCONHEt cf3 Cl Cl NCONHPr cf3 Cl Cl nconh2 cf3 Cl Cl NCONHMe cf3 Cl Cl NCN cf3 Cl Cl NCOSMe cf3 Cl Cl NCOSEt cf3 Cl Cl NCSOMe CF3 Cl Cl NCSOEt cf3 Cl Cl NCSOPr cf3 Cl Cl NSO2NH2 cf3 Cl Cl NSO2NHMe cf3 Cl Cl NSO2NMe2 cf3 Cl Cl NP(O)(OMe)2 cf3 Cl Cl NP(O)(OEt)2 cf3 Cl Cl NP(O)Me2 201 cf3 Cl Cl NP(O)Et2 cf3 Cl Cl NP(O)Me(OMe) cf3 Cl Cl NP(O)(OPr)2 cf3 Cl Cl NC(O)C(O)H cf3 Cl Cl NC(O)C(O)Me cf3 Cl Cl NC(O)C(O)OMe cf3 Cl Cl NC(O)C(O)OEt cf3 Cl Cl NC(O)C(O)NH2 cf3 Cl Cl NC(O)C(O)OH cf3 Cl Cl NC(NH)NH2 cf3 Cl Cl NC(NOH)NH2 cf3 Cl Cl NC(NH)NHMe cf3 Cl Cl NC(NH)NMe2 cf3 Cl Cl NC(NH)OMe cf3 Cl Cl NC(NH)OEt cf3 Cl Cl NCOMe 0 cf3 Cl Cl NCOEt o cf3 Cl Cl NCOPr 0 cf3 Cl Cl NCHO 0 cf3 Cl Cl NCOiPr 0 cf3 Cl Cl NCOtBu 0 cf3 Cl Cl NCOPh 0 cf3 Cl Cl NSO2Me 0 cf3 Cl Cl NSO2Et 0 cf3 Cl Cl NSO2Pr 0 cf3 Cl Cl NSO2Ph 0 cf3 Cl Cl NSO2iPr 0 cf3 Cl Cl nno2 0 202 cf3 Cl Cl NCOOMe 0 cf3 Cl Cl NCOOEt 0 cf3 Cl Cl NCOOPr O cf3 Cl Cl NCOOiPr 0 cf3 Cl Cl NCONHEt 0 cf3 Cl Cl NCONHPr 0 cf3 Cl Cl NCONH2 0 cf3 Cl Cl NCONHMe 0 cf3 Cl Cl NCN 0 cf3 Cl Cl NCOSMe O cf3 Cl Cl NCOSEt 0 cf3 Cl Cl NCSOMe 0 cf3 Cl Cl NCSOEt 0 cf3 Cl Cl NCSOPr 0 cf3 Cl Cl nso2nh2 O cf3 Cl Cl NSO2NHMe 0 cf3 Cl Cl NSO2NMe2 0 cf3 Cl Cl NP(O)(OMe)2 0 cf3 Cl Cl NP(O)(OEt)2 0 cf3 Cl Cl NP(O)Me2 0 cf3 Cl Cl NP(O)Et2 0 cf3 Cl Cl NP(O)Me(OMe) 0 cf3 Cl Cl NP(O)(OPr)2 0 cf3 Cl Cl NC(O)C(O)H 0 cf3 Cl Cl NC(O)C(O)Me 0 cf3 Cl Cl NC(O)C(O)OMe 0 cf3 Cl Cl NC(O)C(O)OEt 0 cf3 Cl Cl NC(O)C(O)NH2 0 203 cf3 Cl Cl NC(O)C(O)OH 0 cf3 Cl Cl NC(NH)NH2 0 cf3 Cl Cl NC(NOH)NH2 0 cf3 Cl Cl NC(NH)NHMe 0 cf3 Cl Cl NC(NH)NMe2 0 cf3 Cl Cl NC(NH)OMe 0 cf3 Cl Cl NC(NH)OEt 0 cf3 Cl H NCOMe cf3 Cl H NCOEt cf3 Cl H NCOPr cf3 Cl H NCHO cf3 Cl H NCOiPr cf3 Cl H NCOtBu cf3 Cl H NCOPh cf3 Cl H NSO2Me cf3 Cl H NSO2Et cf3 Cl H NSO2Pr cf3 Cl H NSO2Ph cf3 Cl H NSO2iPr cf3 Cl H nno2 cf3 Cl H NCOOMe cf3 Cl H NCOOEt cf3 Cl H NCOOPr cf3 Cl H NCOOiPr cf3 Cl H NCONHEt cf3 Cl H NCONHPr cf3 Cl H nconh2 cf3 Cl H NCONHMe 204 cf3 Cl H NCN cf3 Cl H NCOSMe cf3 Cl H NCOSEt cf3 Cl H NCSOMe cf3 Cl H NCSOEt cf3 Cl H NCSOPr cf3 Cl H NSO2NH2 cf3 Cl H NS02NHMe cf3 Cl H NSO2NMe2 cf3 Cl H NP(O)(OMe)2 cf3 Cl H NP(O)(OEt)2 cf3 Cl H NP(O)Me2 cf3 Cl H NP(O)Et2 cf3 Cl H NP(O)Me(OMe) cf3 Cl H NP(O)(OPr)2 cf3 Cl H NC(O)C(O)H cf3 Cl H NC(O)C(O)Me cf3 Cl H NC(O)C(O)OMe cf3 Cl H NC(O)C(O)OEt cf3 Cl H NC(O)C(O)NH2 cf3 Cl H NC(O)C(O)OH cf3 Cl H NC(NH)NH2 cf3 Cl H NC(N0H)NH2 cf3 Cl H NC(NH)NHMe cf3 Cl H NC(NH)NMe2 cf3 Cl H NC(NH)0Me cf3 Cl H NC(NH)OEt cf3 Cl H NCOMe 205 cf3 Cl H NCOEt 0 cf3 Cl H NCOPr 0 cf3 Cl H NCHO 0 cf3 Cl H NCOiPr 0 cf3 Cl H NCOtBu 0 cf3 Cl H NCOPh 0 cf3 Cl H NSO2Me 0 cf3 Cl H NSO2Et 0 cf3 Cl H NSO2Pr O cf3 Cl H NSO2Ph 0 cf3 Cl H NSO2iPr 0 cf3 Cl H NNO2 0 cf3 Cl H NCOOMe 0 cf3 Cl H NCOOEt 0 cf3 Cl H NCOOPr O cf3 Cl H NCOOiPr 0 cf3 Cl H NCONHEt O cf3 Cl H NCONHPr 0 cf3 Cl H NCONH2 0 cf3 Cl H NCONHMe 0 cf3 Cl H NCN 0 cf3 Cl H NCOSMe 0 cf3 Cl H NCOSEt 0 cf3 Cl H NCSOMe 0 cf3 Cl H NCSOEt 0 cf3 Cl H NCSOPr 0 cf3 Cl H NSO2NH2 0 cf3 Cl H NSO2NHMe 0 206 CF3 Cl H NSO2NMe? 0 cf3 Cl H NP(O)(OMe)2 0 cf3 Cl H NP(O)(OEt)2 0 cf3 Cl H NP(O)Me2 0 cf3 Cl H NP(O)Et2 0 cf3 Cl H NP(O)Me(OMe) 0 cf3 Cl H NP(O)(OPr)2 O cf3 Cl H NC(O)C(O)H O cf3 Cl H NC(O)C(O)Me O cf3 Cl H NC(O)C(O)OMe 0 cf3 Cl H NC(O)C(O)OEt 0 cf3 Cl H NC(O)C(O)NH2 0 cf3 Cl H NC(O)C(O)OH 0 cf3 Cl H NC(NH)NH2 0 cf3 Cl H NC(NOH)NH2 0 cf3 Cl H NC(NH)NHMe 0 cf3 Cl H NC(NH)NMe2 O cf3 Cl H NC(NH)OMe 0 cf3 Cl H NC(NH)OEt 0 207

COMPOSITIONS AND METHODS OF USE

The present invention provides pesticidal compositions and methods of controlling arthropod, nematode, helminth and protozoan pests, using the compounds of formulas (I) and (II), as set forth in the Summary of the Invention hereinabove. In a preferred aspect, the present invention provides a method for controlling arthropods or nematodes at a locus comprising applying to said locus an arthropodicidally or nematocidally effective amount of a compound of either formula (I) or formula (II) or a composition comprising said compound and an agriculturally acceptable inert carrier therefor. In a more preferred embodiment, the arthropods whose control is desired are insects, and to that end the invention provides a method for controlling insects at a locus comprising applying to said locus an insecticidally effective amount of a compound of either formula (I) or (II), or an insecticidally effective amount of an insecticidal composition comprising an insecticidally effective amount of a compound of either formula (I) or (II) and an agriculturally acceptable inert carrier therefor.

In another preferred embodiment, control of nematodes is desired, and to that end the invention provides a method of controlling nematodes at a locus comprising applying to said locus a nematocidally effective amount of a compound of either formula (I) or (Π), or a nematocidally effective amount of a nematocidal composition comprising a nematocidally effective amount of a compound of either formula (I) or (II) and an agriculturally acceptable inert carrier therefor. Preferably, the locus to which the arthropodicidally (especially insecticidally) or nematocidally effective amount is applied is a crop-growing area, that is, an area in which a crop is growing or in which a crop has been planted, or an area in which a crop will be planted/grown.

The compositions which can be used in the invention for the pesticidal, particularly the arthropodicidal (especially insecticidal) or nematocidal, treatment of the invention can comprise from about 0.001 to about 95% of the active ingredient of either formula (I) or (II). The term "active ingredient of either formula (I) or (Π)" or "active ingredient" as used herein refers to a compound of either formula (I) or (II) or salt thereof. The expression "compound of either formula (I) or (Π)" is also used herein to mean the compound or its salt.

The diluted liquid formulations, as applied to the locus to be treated or crop, generally comprise from about 0.001 to about 3% of active ingredient of either formula (I) or (II), preferably from about 0.1 to about 0.5%. 208

The solid formulations as applied to the locus or crop generally comprise from about 0.1 to about 8% of active ingredient of either formula (I) or (II), preferably from about 0.5 to about 1.5%.

The concentrated compositions are compositions which are commercialized or transported or stored. For application to plants, they are normally diluted in water and applied in such diluted form. The diluted forms are part of the invention as well as the concentrated forms.

The concentrated formulations generally comprise from about 5 to about 95% of active ingredient of either formula (I) or (Π), preferably from about 10 to about 50%.

The insecticidal compositions of the invention can be applied once, or more than once, throughout the whole insect season. Insecticidal compositions according to the invention are usually applied to the locus to be treated or crop area at a rate of from about 0.04 to about 2 kg/ha of active ingredient, preferably from about 0.1 to about 1 kg/ha.

The concentrated insecticidal compositions according to the invention can be in the form of a solid, e.g., dusts or granules or wettable powders, or, preferably, in the form of a liquid, such as an emulsifiable concentrate or a true solution.

The compositions according to the instant invention generally comprise from about 0.5 to about 95% of active ingredient. The remainder of the composition up to 100% comprises a carrier as well as various additives such as those hereafter indicated.

By "carrier", there is meant herein an organic or inorganic material, which can be natural or synthetic, and which is associated with the active ingredient and which facilitates its application to the locus to be treated or crop. This carrier is thus generally inert and should be agriculturally acceptable, especially on the contemplated or treated locus or crop. The carrier can be solid (clay, silicates, silica, resins, wax, fertilizers, etc.) or liquid (water, alcohols, ketones, oil solvents, saturated or unsaturated hydrocarbons, chlorinated hydrocarbons, liquified petroleum gas, etc.).

Among the many additives, the compositions of the invention can comprise surfactants as well as other ingredients such as dispersants, stickers, antifoam agents, antifreezing agents, dyestuffs, thickeners, adhesives, protective colloids, penetrating agents, stabilizing agents, sequestering agents, antiflocculating agents, corrosion inhibitors, pigments and polymers.

More generally, the compositions of the invention can comprise all kinds of solid or liquid additives which are known in the art of insecticides and insecticidal treatments. 209

The surfactants can be of the emulsifying or wetting type, ionic or non-ionic.

Possible surfactants are salts of polyacrylic or lignosulfonic acids; salts of phenolsulfonic or naphthalenesulfonic acids; polycondensates of ethylene oxide with fatty alcohols or fatty acids or fatty amines or substituted phenols (particularly alkylphenols or arylphenols); ester-salts of sulfosuccinic acids; taurine derivatives such as alkyl taurates; phosphoric esters; or esters of alcohols or polyoxyethylated phenols. When the spraying vehicle is water, the use of at least one surfactant is generally required because the active ingredients are not water-soluble.

The method of application of the compositions of the invention is generally the spraying of a mixture which has been previously made by dilution of more concentrated formulations according to the invention.

Solid compositions can be powders for dusting or for dispersion (wherein the content of active ingredient can be up to 100%) and granules, especially extruded or compacted granules, or granules which have been made by impregnation of a powder (the content of active ingredient in such powders can then be between about 1 and about 80%).

Liquid compositions or compositions which have to be liquid when applied include solutions, water-soluble concentrates, emulsifiable concentrates, emulsions, wettable powders or pastes or water-dispersible granules.

Emulsifiable concentrates generally comprise from about 10 to about 80% of active ingredient; the emulsions when applied generally comprise from about 0.01 to about 20% of active ingredient.

For example, the emulsifiable concentrates can comprise the solvent and, to the extent needed, from about 2 to about 20% of suitable additives as stabilizers, surfactants, penetrating agents, corrosion inhibitors or other additives already recited.

These concentrates are usually diluted in tank water so as to obtain the dilution appropriate for spraying.

The concentrated suspensions can also be applied by spraying and have to be fluid without allowing any solid to separate and fall to the bottom. Generally they comprise from about 1 to about 75% of active ingredient (preferably from about 2 to about 50%), from about 0.5 to about 15% of surfactants, from about 0.1 to about 10% of thickener, and from 0 to about 10% of other suitable additives as already indicated, the remainder being water or an organic liquid wherein the active ingredient is insoluble or has a low solubility. 210

The wettable powders generally comprise the active ingredient (from about 1 to about 95%, preferably from about 2 to about 80%), the solid carrier, a wetting agent (from 0 to about 5%), a dispersing agent (from about 3 to about 10%) and, to the extent needed, from 0 to about 10% of other additives such as stabilizers and others as already listed.

In order to obtain these wettable powders or dusting powders, it is appropriate to intimately mix the active ingredients and the additives, as by grinding in a mill or similar device.

Dispersible granules are generally made by agglomeration of a powder followed by an appropriate granulation process.

The emulsions herein described can be of the oil-in-water or water-in-oil types. Fluidity of the emulsions can range from low viscosities up to high viscosities approaching those of gels.

Among these many compositions or formulations, one skilled in the art can choose the one most appropriate, according to the specific conditions of the treatment problem.

The compounds and compositions of the invention can also be used in admixtures with another pesticide e.g., an insecticide, acaricide or herbicide.

The invention is further illustrated by the following examples which are not considered as limiting the invention but are given to better enable use of it.

BIOLOGICAL EFFICACY

The following representative methods were used to apply the compounds of the invention and to observe the biological activity obtained therefrom: a soil drench on aphid-infested plants; a bait application on flies.

The species used were as follows:

GENUS, SPECIES

COMMON NAME

Aphis gossypii Schizaphis graminum Musca domestica cotton leaf aphid greenbug housefly

The Soil Drench Test (systemic activity: aphids)

Cotton and sorghum plants were established in pots. One day prior to treatment, each pot was infested with about 25 aphids of a mixed population. Cotton plants were infested with aphids and sorghum plants were infested with the greenbug. The selected compound of 1 211 formula (I) or formula (II) was applied to the soil surface in a dilution that delivered the equivalent of 10.0 ppm soil concentration by weight. Aphid counts were obtained at 5 DAT (i.e. days after treatment). The number of aphids on the treated plants was compared to the number of those on the untreated control plants. Compounds that showed greater than 30% 5 mortality on either aphid or greenbug were the following: la, lb, 3-29, 30a, 31-32

The Housefly Bait/Contact Test

About 25 four to six-day-old adult houseflies (Musca domestica) were anesthetized and placed in a cage with a sugar water bait solution containing the compound. The compound 10 concentration in the bait solution was 100 ppm. After 24 hours, flies which showed no movement on stimulation were considered dead. Compounds that showed greater than 30% mortality on housefly were the following: 1, la, lb, 2, 3-10, 12-14, 16, 18-20,22,25,26, 28-30, 30a, 31, 32

While the invention has been described in terms of various preferred embodiments, the skilled artisan will appreciate that various modifications, substitutions, omissions and changes can be made without departing from the spirit thereof. Accordingly, it is intended 2 0 that the scope of the present invention be limited solely by the scope of the following claims, including equivalents thereof.