4.5 Article

Highly efficient synthesis of vinyl substituted triazoles by Au(I) catalyzed alkyne activation

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 14, Pages 3899-3902

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.03.096

Keywords

1,2,3-Triazoles; Au catalysis; Alkyne activation; Regioselective; Stereoselective

Funding

  1. ACS-PRF

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Au(I) catalyzed 1,2,3-triazole addition to non-activated alkyne was reported. A large group of substituted NH-1,2,3-triazoles were suitable for this transformation along with both internal and terminal alkynes. The N-1 and N-2 vinyl substituted 1,2,3-triazoles were prepared in up to 98% yield with as low as 0.2% catalyst loading, thereby providing a new protocol for the synthesis of potentially biological-active vinyl-triazole building blocks. (C) 2009 Elsevier Ltd. All rights reserved.

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