Parallel synthesis of 1,2,4-oxadiazoles from carboxylic acids using an improved, uronium-based, activation

被引:82
作者
Poulain, RF
Tartar, AL
Déprez, BP
机构
[1] Fac Sci & Pharmaceut & Biol, Chim Organ Lab, UMR 8525, F-59006 Lille, France
[2] Devgen nv, B-9052 Ghent, Belgium
关键词
D O I
10.1016/S0040-4039(00)02293-0
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
We describe the synthesis of 1,2,4-oxadiazoles from carboxylic acids and amidoximes using 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate (TBTU) as an activating agent of the carboxylic acid function for the O-acylation step. This method was used for the synthesis of a library of 24 1,2,4-oxadiazoles. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1495 / 1498
页数:4
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