Copper-Catalyzed Direct Amination of 1,2,3-Triazole N-Oxides by C-H Activation and C-N Coupling

An efficient approach for the synthesis of 4-amino-2-aryl-1,2,3-triazole derivatives has been developed through the copper-catalyzed direct C-H amination of 2-aryl-1,2,3-triazole N-oxides under mild reaction conditions. Various amines, including primary and secondary aliphatic and aromatic amines, can be employed as effective coupling partners. The general performance of our method was also demonstrated by the oxidative amination of thiazole and imidazole N-oxides.