Syngas as a synergistic reducing agent for selective reductive amination—a mild route to bioactive amines

Abstract

Current approaches to the reductive amination are often nonselective, require complicated catalysts, or are not atom-economical. The application of syngas as a mild and selective reducing agent to aminate carbonyl compounds unstable under hygrogenation conditions with functional groups, which furnished a broad substrate scope, is demonstrated herein. Amino acid precursor and furfurylamine derivative were prepared indicating the high selectivity of the protocol. Several products with antifungal activity higher than triadimefon were synthesized.