The reaction of ?-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 involve in situ formation of ?-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.