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Regiospecific Synthesis of 1,4,5-Trisubstituted-1,2,3-triazole via One-Pot Reaction Promoted by Copper(I) Salt

Yong-Ming Wu*, Juan Deng, Ya Li, Qing-Yun Chen

*Chinese Academy of Sciences, 354 Fenglin Rd., Shanghai 200032, P. R. China, Email:

Y.-M. Wu, J. Deng, Y. L. Li, Q.-Y. Chen, Synthesis, 2005, 1314-1318.

DOI: 10.1055/s-2005-861860

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A method for the regiospecific synthesis of 1,4,5-trisubstituted-1,2,3-triazole catalyzed by copper(I) iodide was developed. This is the first example of a regiospecific synthesis of 5-iodo-1,4-disubstituted-1,2,3-triazole, which can be further elaborated to a range of 1,4,5-trisubstituted-1,2,3-triazole derivatives.

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Key Words

fluoroalkyl-1,4,5-trisubstituted-1,2,3-triazoles, 1,2,3-triazoles, one-pot reaction, regiospecific synthesis, fluoroalkylazide, terminal alkyne, cycloaddition, heterocycles, iodination

ID: J66-Y2005-790