A Concise Asymmetric Synthesis of the Potent Enkephalinase Inhibitor Kelatorphan

Abstract

A concise asymmetric synthesis of the enkephalinase inhibitor Kelatorphan has been completed in seven steps from commercially available hydrocinnamyl chloride. The synthesis features as a key step an asymmetric C-C bond formation which utilizes Oppolzer bornane-sultam alkylation methodology.