Patent ID: 6369194
Filing Date: 2002-04-09
Classification: C07D

Abstract:
A method for preparing a vicinyl tricarbonyl compound of the general formula: where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, alcohols, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, by removal of a H atom selected from the group consisting of amines, amino acids, peptides, water, hydrogen sulfide, alcohols, and thiols, which comprises:reacting an &agr;-keto acid or an acid chloride of an &agr;-keto acid with a ylide, wherein said ylide is selected from (cyanomethylene)phosphoranes and triphenyl phosphoranes, to form a cyano diketo phosphorane; oxidizing the cyano diketo phosphorane to form a cyano tricarbonyl; and reacting the cyano tricarbonyl with a nucleophile, NuH, as described above, to form said vicinyl tricarbonyl compound.