Enzyme-Catalyzed Regioselective Synthesis of 4-Hetero-Functionalized 1,5-Disubstituted 1,2,3-Triazoles

Enzyme-catalyzed novel protocols for the regioselective construction of fully substituted 1,2,3-triazoles by employing 2-azido-1,3,5-triazine (ADT) as a 1,3-dipole for the cycloaddition reaction with the activated alkene in an aqueous medium have been developed. Various 4-heterosubstituted-1,2,3-triazoles were readily assembled in good to excellent yields with high regioselectivity. This reaction also features wide substrate scope, strong functional group tolerance, gram-scale synthesis, and an environmentally friendly process.