Regioselective Conversion of Arenes to N-aryl-1,2,3-triazoles Using CH Borylation

A one-pot protocol for the synthesis of N-aryl 1,2,3-triazoles from arenes by an iridium-catalyzed CH borylation/copper catalyzed azidation/click sequence is described. 1mol% of Cu(OTf)2 was found to efficiently catalyze both the azidation and the click reaction. The applicability of this method is demonstrated by the late-stage chemoselective installation of 1,2,3-triazole moiety into unactivated molecules of pharmaceutical importance.