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钯催化通过C-H官能化/分子内C-S键形成过程合成2-取代苯并噻唑

Palladium-catalyzed synthesis of 2-substituted benzothiazoles via a C-H functionalization/intramolecular C-S bond formation process.

作者信息

Inamoto Kiyofumi, Hasegawa Chisa, Hiroya Kou, Doi Takayuki

机构信息

Graduate School of Pharmaceutical Sciences, Tohoku University, Aramaki, Sendai, Japan.

出版信息

Org Lett. 2008 Nov 20;10(22):5147-50. doi: 10.1021/ol802033p. Epub 2008 Oct 24.

Abstract

Catalytic synthesis of 2-substituted benzothiazoles from thiobenzanilides was achieved in the presence of a palladium catalyst through C-H functionalization/C-S bond formation. This method features the use of a novel catalytic system consisting of 10 mol % of Pd(II), 50 mol % of Cu(I), and 2 equiv of Bu4NBr that produced variously substituted benzothiazoles in high yields with good functional group tolerance.

摘要

在钯催化剂存在下,通过C-H官能化/C-S键形成反应实现了由硫代苯甲酰苯胺催化合成2-取代苯并噻唑。该方法的特点是使用了一种新型催化体系,该体系由10 mol%的Pd(II)、50 mol%的Cu(I)和2当量的Bu4NBr组成,能够以高收率和良好的官能团耐受性制备各种取代的苯并噻唑。

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