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Two classes of 1,4-disubstituted 1,2,3-triazoles were synthesized using one-pot reaction of α-tosyloxy ketones/α-halo ketones, sodium azide, and terminal alkynes in the presence of aq PEG (1:1, v/v) using the click chemistry approach and evaluated for Src kinase inhibitory activity. Structure-activity relationship analysis demonstrated that insertion of C(6)H(5)- and 4-CH(3)C(6)H(4)- at position 4 for both classes and less bulkier aromatic group at position 1 in class 1 contribute critically to the modest Src inhibition activity (IC(50) = 32-43 μM) of 1,4-disubstituted 1,2,3-triazoles.

An efficient, one-pot, regioselective synthesis of 1,4-diaryl-1H-1,2,3-triazoles is described via the copper(I)-catalyzed reaction of diaryliodonium salts, sodium azide and terminal alkynes. The generality of this protocol is demonstrated by the synthesis of a series of 1,4-diaryl-1H-1,2,3-triazoles in good to high yields. The catalyst and reaction solvent are reused without any appreciable reduction in product yield.