An efficient phosphine-free palladium coupling for the synthesis of new 2-arylbenzo[b]thiophenes
An efficient phosphine-free palladium coupling for the synthesis of new 2-arylbenzo[b]thiophenes
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DOI：
10.1016/j.tet.2004.02.011
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发表时间：
2004-03-29
期刊：
影响因子：
2.1
通讯作者：
Lemaire, M
中科院分区：
文献类型：
--
作者：
Chabert, JFD;Joucla, L;Lemaire, M
已经开发出直接、快速获取 2-芳基苯并[b]噻吩的方法。它涉及在无膦钯体系存在下，3-活化苯并[b]噻吩与几种芳基卤化物的催化偶联。对于醛等脆弱官能团，与其他底物一样使用季铵作为添加剂，在冠醚存在下偶联效果更好更快，最好的是DCH-18-C-6，具有良好的收率和较短的反应时间。该方法将提供对具有生物学意义的新颖结构的直接访问。 (C) 2004 Elsevier Ltd. 保留所有权利。
Straightforward and rapid access to 2-arylbenzo[b]thiophenes has been developed. It involved a catalytic coupling of 3-activated benzo[b]thiophenes with several aryl halides in the presence of a phosphine-free palladium system. In case of fragile functional groups such as aldehydes, a quaternary ammonium was used as an additive as with the other substrates, the coupling performed better and faster in the presence of a crown ether, the best one being DCH-18-C-6, with good yields and low reaction times. This method would provide a direct access to novel structures of biological interest. (C) 2004 Elsevier Ltd. All rights reserved.