Metal-free 1,3-dipolar cyclization of azides with HFO-1233zd(E) in the presence of amines: one-step regioselective synthesis of 1-N-substituted 1,2,3-triazole-4-carboxamide derivatives

Abstract

A simple and metal-free strategy for the regioselective synthesis of 1-N-substituted 1,2,3-triazole-4-carboxamide derivatives was developed by employing azides, HFO-1233zd(E) and amines in an aqueous reaction medium. The defluorinative functionalization of the C(sp³)–F bond in the trifluoromethyl group into amides was involved in the reaction process.