Three-Component Copper-Catalyzed 1,4-Carboamination of 1,3-Dienes

We herein report a highly selective copper-catalyzed three-component 1,4-carboamination of 1,3-dienes with activated alkyl bromides and amines, providing a general and practical route to functionalized allylamine derivatives. This operationally simple protocol demonstrates a broad substrate scope (>45 examples), good functional group tolerance, and high E/Z ratio selectivity. The synthetic utility of this method was further exemplified by its successful application in the late-stage functionalization of various bioactive molecules.