A facile and regioselective synthesis of 1,4-disubstituted 1,2,3-triazoles using click chemistry

The reaction of α-tosyloxy ketones, sodium azide, and terminal alkynes in presence of copper(I) in aqueous polyethylene glycol afforded regioselectively 1,4-disubstituted 1,2,3-triazoles in good yield at ambient temperature. The one-pot exclusive formation of 1,4-disubstituted 1,2,3-triazoles involves in situ formation of α-azido ketones, followed by cycloaddition reaction with terminal alkyne. The generality of this one-pot method was demonstrated by synthesizing an array of diverse 1,4-disubstituted 1,2,3-triazoles.