Scandium-catalyzed highly selective N2-alkylation of benzotriazoles with cyclohexanones

Abstract

A scandium-catalyzed highly N²-selective alkylation of benzotriazoles with cyclohexanones has been developed, providing straightforward access to a series of N²-alkylated benzotriazoles featuring newly formed tetrasubstituted carbon centers in high yields with excellent regioselectivities. The key to the success of this reaction is using Sc(OTf)₃ as the catalyst. Typically, this protocol is also well compatible with 4-aryl-1,2,3-triazoles.