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一种从异腈和二溴芳基磺酰胺合成异脲和异硫脲的统一方法。

A Unified Approach for the Synthesis of Isourea and Isothiourea from Isonitrile and -Dibromoarylsulfonamides.

机构信息

Department of Chemistry, Gauhati University, Guwahati, Assam 781014, India.

出版信息

J Org Chem. 2021 Dec 17;86(24):17581-17593. doi: 10.1021/acs.joc.1c01578. Epub 2021 Dec 2.

Abstract

A unified approach has been developed for the synthesis of both isourea and isothiourea in a three-component coupling reaction by treating alcohols or thiols respectively with -dibromoarylsulfonamides and isonitrile and in the presence of KCO. This metal-free process proceeds via carbodiimide intermediate at room temperature within a very short reaction time. A library of sulfonylisoureas and isothioureas has been made using this synthetic protocol with wide substrate scope in good to high yields.

摘要

已开发出一种用于三组分偶联反应中合成异脲和异硫脲的统一方法,该方法分别通过 - 二溴芳基磺酰胺和异腈处理醇或硫醇,并在 KCO 的存在下进行。该无金属过程在室温下通过碳二亚胺中间体在很短的反应时间内进行。使用这种合成方案,已经制备了包含磺酰基异脲和异硫脲的文库,具有广泛的底物范围,产率良好至高产率。

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