ABSTRACT
A facile and efficient method for the regioselective acetoxylation of 1-benzyl 1,2,3-triazoles through C–H bond activation was developed. Cu(OAc)2 and 1,2,3-triazole were applied as catalyst and elegant directing group, respectively, to convert aromatic C–H bonds directly into highly regioselective C–O bonds. The conversion can result in the synthesis of 1,2,3-triazoles bearing acetoxyl groups.