Ag-Catalyzed minisci C-H difluoromethylarylation of N-heteroarenes.,Organic & Biomolecular Chemistry

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Ag-Catalyzed minisci C-H difluoromethylarylation of N-heteroarenes.
Organic & Biomolecular Chemistry ( IF 2.9 ) Pub Date : 2020-01-07 , DOI: 10.1039/c9ob02586c
Xiaojuan Xie ₁ , Yifang Zhang , Jian Hao , Wen Wan

Affiliation

A mild silver-catalyzed decarboxylative difluoromethylarylation of electron-deficient N-heteroarenes has been developed by using aryldifluoro acetic acid as difluoromethyl sources. This protocol provides an efficient and straightforward access to difluoromethylated heteroarenes in moderate to excellent yields with good selectivities. Furthermore, this reaction was applicable to bioactive heteroarenes, providing a straightforward approach for the late-stage C-H difluoromethylation of pharmacophores.

中文翻译：

Ag催化的N-杂芳烃的Minisci CH二氟甲基芳基化。

通过使用芳基二氟乙酸作为二氟甲基源，开发了电子缺陷型N-杂芳烃的温和银催化的脱羧二氟甲基芳基化反应。该方案以中等至优异的收率和良好的选择性，提供了对二氟甲基化杂芳烃的高效直接访问。此外，该反应适用于生物活性杂芳烃，为药效基团的后期CH二氟甲基化提供了直接的方法。

更新日期：2020-01-07

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