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One-Pot Three-Step Synthesis of 1,2,3-Triazoles by Copper-Catalyzed Cycloaddition of Azides with Alkynes formed by a Sonogashira Cross-Coupling and Desilylation

Férdéric Friscourt and Geert-Jan Boons*

*Complex Carbohydrate Research Center, University of Georgia, 315 Riverbend Road, Athens, Georgia 30602, United States, Email: gjboonsccrc.uga.edu

F. Friscourt, G.-J. Boons, Org. Lett., 2010, 12, 4936-4939.

DOI: 10.1021/ol1022036 (free Supporting Information)


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Abstract

A microwave-assisted, one-pot, three-step Sonogashira cross-coupling-desilylation-cycloaddition sequence enables a convenient preparation of 1,4-disubstituted 1,2,3-triazoles starting from a range of aryl halides, aroyl chlorides, ethynyltrimethylsilane, and azides.

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Key Words

Microwave Synthesis, Click Chemistry, Sonogashira Coupling


ID: J54-Y2010-3120