A rapid and efficient route to benzazole heterocycles

被引：0
|
作者：
Richard D Carpenter
Mark J Kurth
机构：
[1] University of California,Department of Chemistry
[2] Present address: Department of Biomedical Engineering,undefined
[3] University of California,undefined
[4] Davis,undefined
[5] California,undefined
[6] USA.,undefined
来源：
Nature Protocols | 2010年 / 5卷
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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 ∼8.5 h to complete: 1–3 h for setup, 4.5 h for benzazole formation and 2 h for workup and purification.
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页码：1731 / 1736
页数：5
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