A copper(l)-catalyzed three-component reaction to form (1 -substituted- 1H- 1,2,3-triazol-4-ylmethyl)-dialkylamines based on the Huisgen cycloaddition using amine, propargyl halide and azide in water was proposed. The process showed considerable synthetic advantages in terms of high atom economy, low environmental impact, atmospheric oxygen, wide substrate scope, mild reaction condition and good yields. (c) 2005 Published by Elsevier Ltd.
One-Pot Synthesis of 1,4-Disubstituted 1,2,3-Triazoles from In Situ Generated Azides
作者:Alina K. Feldman、Benoît Colasson、Valery V. Fokin
DOI:10.1021/ol048859z
日期:2004.10.1
[reaction: see text] 1,4-Disubstituted1,2,3-triazoles are obtained in excellent yields by a convenient one-pot procedure from a variety of readily available aromatic and aliphatic halides without isolation of potentially unstable organic azide intermediates.