Ni-catalyzed synthesis of 1,5-disubstituted 1,2,3-triazoles

Abstract

Regioselective 1,4-disubstituted triazoles have been accessed particularly using copper-catalyze azide-alkyne cycloaddition.[1] In sharp contrast, the synthetic methods to afford 1,5-disubstituted compounds have been developed relatively slowly. Ruthenium- and lanthanide-based catalytic reactions have been practically limited due to the air- and moisture sensitivities. Herein, we unveil nickel-catalyzed highly selective 1,5-disubstituted triazole formation reaction under the ambient conditions.[2] In particular, the reaction protocol is compatible with organic solvent and aqueous solvent conditions, which can be potentially applied to the biochemical approaches.