K2CO3-promoted synthesis of amides from 1-aryl-2,2,2-trifluoroethanones and amines under mild conditions

Abstract

A base-promoted amidation of 1-aryl-2,2,2-trifluoroethanones with amines via Haller–Bauer reaction has been developed. In this reaction, the direct transformation of 1-aryl-2,2,2-trifluoroethanones into amides via C(O)–C bond cleavage occurs without the use of any stoichiometric chemical oxidants or transition-metal catalysts. A series of primary and secondary amines are shown to be compatible with this transformation, and several pharmaceutical molecules were synthesized.