Synthesis of 5‐Trifluoromethyl‐1,2,4‐Triazoles via Palladium‐Catalyzed [4 + 1] Oxidative Annulation of Trifluoroacetimidohydrazides and Isocyanides

A Pd‐catalyzed aerobic oxidative annulation of trifluoroacetimidohydrazides and isocyanides has been developed, offering an efficient and straightforward access to valuable 1,2,4‐triazoles with both trifluoromethyl and amino functionality. The reaction proceeds smoothly with catalytic Pd(OAc) 2 without an additional ligand, which features simple operation, low catalyst loading, high efficiency, and scalability. In this transformation, isocyanide serves as the C1 and amino source.