Enantioselective benzoylation of alpha-amino esters using (S)-1-benzoyl-2- (alpha-acetoxyethyl)benzimidazole, a chiral benzimidazolide.

A new chiral benzimidazolide is developed as a nonenzymatic acylating agent for enantioselective benzoylation of racemic alpha-amino esters. The process is highly efficient, which exhibits uniformly high enantioselectivity for alpha-amino esters with or without aryl substituents under mild reaction conditions. The chiral benzimidazolide is inexpensive and is easily accessible.