A convergent synthesis of alpha-aryl-beta ketonitriles

The invention relates to the general and the convergent synthesis of the present invention wherein the 3-unsubstituted-4-arylisoxazole promoted isomerization and the resulting enolate acidification give the a-aryl-b-ketonitriles of the title. The corresponding 3-unsubstituted-4-arylisoxazoles are prepared by reaction of 4-iodo-5-substituted dithoxazoles or 4-bromo-5-substituted isoxazoles and arylborosaccharides in the presence of a suitable catalyst. The a-aryl-b-ketonitriles of the present invention serve as a synthetic linkage product for the synthesis of biologically important compounds, for example, anortic antagonists of the kortikotropin releasing factor (CRF) receptor. HE