Palladium-catalyzed carbonylative synthesis of 5-trifluoromethyl-1,2,4-triazoles from trifluoroacetimidohydrazides and aryl iodides

摘要

A palladium-catalyzed three-component carbonylative reaction of trifluoroacetimidohydrazides and aryl iodides for the synthesis of pharmaceutically valuable 5-trifluoromethyl-1,2,4-triazoles has been achieved. The reaction is characterized by a low catalyst loading amount, a broad substrate scope, high efficiency, no participation of CO gas and good application prospects. The protocol has been successfully applied to prepare the bioactive molecule GlyT1 inhibitor.