Abstract

Chemoselective acylation of amines has been carried out in water under open air using acyclic or cyclic anhydrides or benzoyl chloride in the absence of any acid or base catalyst or a surfactant. The alkyl or aryl amines including primary or secondary amines, amino acids, diamines etc afforded the corresponding N-acyl derivatives in good yields. The selective N-acylation was observed in the presence of -OH, -SH, -COOH or -COOEt group. Being a practical alternative to the existing methods for selective acylation of amines the present methodology may find applications.

Keywords: Acylation, amines, anhydrides, water.