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

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.

Automated summary

Current approaches to reductive amination lack selectivity, require complex catalysts, or are not atom-economical. This study demonstrates the use of syngas as a mild and selective reducing agent for aminating carbonyl compounds with functional groups that are unstable under hydrogenation conditions. The method has a broad substrate scope and amino acid precursor and furfurylamine derivative were prepared, showing high selectivity. Several products with antifungal activity higher than triadimefon were synthesized.