作者
Christian W Tornøe, Morten Meldal
发表日期
2001/6/9
图书
Peptides: The Wave of the Future: Proceedings of the Second International and the Seventeenth American Peptide Symposium, June 9–14, 2001, San Diego, California, USA
页码范围
263-264
出版商
Springer Netherlands
简介
[1,2,3]-Triazoles are important pharmacophores in medicinal chemistry and it is therefore important to develop synthetic methods for triazoles that are both mild, high yielding and applicable to combinatorial synthesis. [1,2,3]-Triazoles are typically prepared by refluxing an alkyne and an azide in toluene (110 °C), but the 1,3-dipolar cycloaddition has also been performed at lower temperatures by using sodium acetylide [1], lithium and magnesium acetylide [2,3] with varying success. The present work describes the preparation of [1,2,3]-triazoles at 25 °C on solid-phase with high yields (80–95%), and is compatible with Fmoc chemistry.
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CW Tornøe, M Meldal - Peptides: The Wave of the Future: Proceedings of the …, 2001