Catalyst-Free Regioselective N² Arylation of 1,2,3-Triazoles Using Diaryl Iodonium Salts

Abstract

The widespread application of 1,2,3-triazoles in pharmaceuticals has resulted in substantial interest toward developing efficient postmodification methods. Whereas there are many postmodification methods available to obtain N¹-substituted 1,2,3-triazoles, developing a selective and convenient protocol to synthesize N²-aryl-1,2,3-triazoles has been challenging. We report a catalyst-free and regioselective method to access N²-aryl-1,2,3-triazoles in good to excellent yields (66-97%). This scalable postmodification protocol is effective for a wide range of substrates.