Background: 1,2,3-Triazoles represent an important structural motif frequently found in organic
chemistry, biological science, medicinal chemistry, and material science. Thus, the synthesis of
novel 1,2,3-triazoles derivatives by an efficient method has attracted considerable attention.
Methods: In this paper, we developed a simple and efficient azidation system of biphenyl tosylhydrazones
with sodium azide. A series of new 4-(1-azidoethyl)-1,1'-biphenyl derivatives were prepared by the metalfree
reductive reaction and further reacted with aryl acetylenes to afford novel 1,4-substituted 1,2,3-
triazoles by water-soluble (salicyladimine)2
Cu complex catalyzed azide-alkyne cycloaddition in water.
Results: The desired 1,4-substituted 1,2,3-triazoles were obtained in 27-94% yields in pure water
without any organic solvent or phase transfer agents.
Conclusion: The catalytic system presented here enables the use of easily accessible starting materials
and good functional group tolerance.