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A Stepwise Huisgen Cycloaddition Process: Copper(I)-Catalyzed Regioselective “Ligation” of Azides and Terminal Alkynes

Vsevolod V. RostovtsevDepartment of Chemistry and the Skaggs Institute for Chemical Biology, The Scripps Research Institute, BCC-315, 10550 N. Torrey Pines Rd., La Jolla, CA 92037, USALuke G. GreenDepartment of Chemistry and the Skaggs Institute for Chemical Biology The Scripps Research Institute, BCC-315 10550 N. Torrey Pines Rd., La Jolla, CA 92037 (USA)Valery V. FokinDepartment of Chemistry and the Skaggs Institute for Chemical Biology The Scripps Research Institute, BCC-315 10550 N. Torrey Pines Rd., La Jolla, CA 92037 (USA) Fax: (+1) 858-784-7562K. Barry SharplessDepartment of Chemistry and the Skaggs Institute for Chemical Biology The Scripps Research Institute, BCC-315 10550 N. Torrey Pines Rd., La Jolla, CA 92037 (USA) Fax: (+1) 858-784-7562
2002en
ABI

Abstract

By simply stirring in water, organic azides and terminal alkynes are readily and cleanly converted into 1,4-disubstituted 1,2,3-triazoles through a highly efficient and regioselective copper(I)-catalyzed process (see scheme for an example). Supporting information for this article is available on the WWW under http://www.angewandte.org or from the author. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2002/2002/z19191_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.

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