Transition metal-free synthesis of 4-trifluoromethyl-1,2,3-triazoles via regioselective (3+2) cycloaddition reactions

The incorporation of a trifluoromethyl group into N-heterocyclic frameworks often imparts significantly enhanced biological activity to the parent compounds. Herein, we report a base-mediated, regioselective (3 + 2) annulation of α-trifluoromethyl ketones with organic azides under transition-metal-free conditions. This protocol provides rapid access to a range of 4-CF3-substituted 1,2,3-triazoles in moderate to good yields and exhibits broad functional group tolerance. The potential applicatons in the synthesis of organic electroluminescent materials and stroke treatment drug highlight the practicality of this method.