A rapid and efficient route to benzazole heterocycles

被引：17

作者：

Carpenter, Richard D. ^{[1
]}

Kurth, Mark J. ^{[1
]}

机构：

[1] Univ Calif Davis, Dept Chem, Davis, CA 95616 USA

来源：

NATURE PROTOCOLS | 2010年 / 5卷 / 11期

基金：

美国国家科学基金会;

关键词：

B-CELL LYMPHOMAS; ALPHA(4)BETA(1) INTEGRIN; DRUG DISCOVERY; BENZIMIDAZOLE; POTENT; BENZOTHIAZOLE; DERIVATIVES; ANTAGONIST; INHIBITORS; DIVERSITY;

D O I：

10.1038/nprot.2010.132

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

This protocol describes a rapid, high-yielding, microwave-mediated route that affords benzazole heterocycles in high crude purity and represents a significant advancement toward an environmentally friendly reaction. The reaction of aryl isothiocyanates with o-nucleophilic anilines produces thiourea intermediates that, in the presence of a carbodiimide-functionalized resin, cyclize to benzazoles with the safe removal of one equivalent of hydrogen sulfide. This procedure takes similar to 8.5 h to complete: 1-3 h for setup, 4.5 h for benzazole formation and 2 h for workup and purification.

引用

页码：1731 / 1736

页数：6

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