Copper‐Catalyzed Direct Synthesis of 1,2,4‐Oxadiazoles from Amides and Organic Nitriles by Oxidative N–O Bond Formation

Abstract

Abstract Herein, we report the first Cu‐catalyzed one‐step method for the synthesis of 1,2,4‐oxadiazoles from stable, less toxic, and readily available amides and organic nitriles by a rare oxidative N–O bond formation using O 2 as sole oxidant. This method has a broad substrate scope and a good tolerance for diverse functional groups. Moreover, the synthetic utility of this method is highlighted by the synthesis of biologically active 3,5‐disubstituted derivatives.