Synthesis of enantiomerically pure α-[4-(1-substituted)-1,2,3-triazol-4-yl]-benzylacetamides via microwave-assisted click chemistry:: towards new potential antimicrobial agents

被引:23
作者
Castagnolo, Daniele [1 ]
Dessi, Filippo [1 ]
Radi, Marco [1 ]
Botta, Maurizio [1 ]
机构
[1] Univ Siena, Dipartimento Farmaco Chim Tecnol, I-53100 Siena, Italy
关键词
D O I
10.1016/j.tetasy.2007.06.007
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
Chiral 1-phenyl-2-propynylamines are important building blocks for the synthesis of antifungal and antiaromatase agents related to bifonazole. In this report, a microwave-assisted Cu(l)-catalyzed 'click chemistry' approach has been employed to easily generate a small library of enantiomerically pure alpha-[4-(1-substituted)- 1,2,3-triazol-4-yl]benzylacetamides starting from racemic propargylamines. These compounds could represent easily accessible intermediates for the synthesis of new antimicrobial agents. (c) 2007 Elsevier Ltd. All rights reserved.
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收藏
页码:1345 / 1350
页数:6
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