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使用三氟氯乙烷通过镍催化进行(杂)芳基溴化物和氯化物的三氟乙基化反应。

Using Chlorotrifluoroethane for Trifluoroethylation of (Hetero)aryl Bromides and Chlorides via Nickel Catalysis.

机构信息

Key Laboratory of Organofluorine Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Lu, Shanghai 200032, China.

Key Laboratory of Biocatalysis & Chiral Drug Synthesis of Guizhou Province, Generic Drug Research Center of Guizhou Province, Zunyi Medical University, Zunyi, Guizhou 563003, P. R. China.

出版信息

Org Lett. 2021 Feb 19;23(4):1400-1405. doi: 10.1021/acs.orglett.1c00058. Epub 2021 Feb 5.

Abstract

A nickel-catalyzed reductive cross-coupling between industrial chemical CFCHCl and (hetero)aryl bromides and chlorides has been reported. The reaction is synthetically simple without the preparation of arylmetals and exhibits high functional group tolerance. The utility of this protocol has been demonstrated by the late-stage modification of pharmaceuticals, providing a facile route for medicinal chemistry.

摘要

报道了一种镍催化的工业化学品 CFCHCl 与(杂)芳基溴化物和氯化物之间的还原交叉偶联反应。该反应合成方法简单,无需制备芳基金属,且对官能团具有高耐受性。该方法在药物的后期修饰中得到了应用,为药物化学提供了一条简便的途径,证明了该方法的实用性。

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