Issue 3, 2020

Ag-Catalyzed minisci C–H difluoromethylarylation of N-heteroarenes

Abstract

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.

Graphical abstract: Ag-Catalyzed minisci C–H difluoromethylarylation of N-heteroarenes

Supplementary files

Article information

Article type
Communication
Submitted
04 Dec 2019
Accepted
19 Dec 2019
First published
19 Dec 2019

Org. Biomol. Chem., 2020,18, 400-404

Ag-Catalyzed minisci C–H difluoromethylarylation of N-heteroarenes

X. Xie, Y. Zhang, J. Hao and W. Wan, Org. Biomol. Chem., 2020, 18, 400 DOI: 10.1039/C9OB02586C

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