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Selective Direct C-H Polyfluoroarylation of Electron-deficient N-heterocycle Compounds

Abstract

The first C2-selective direct C-H polyfluoroarylation of electron-deficient N-heterocycles with polyfluorobenzoic acid via decarboxylative arylation process were achieved by using CuBr2 as the mediator in green solvent diglyme. The key to success is using N-methylation activation strategy and TBAB as an important addtive. The protocol features broad substrate scope, ligand- and base-free conditions, good functional group compatibility, and offers a powerful synthetic tool for assembling various polyfluoroaryl N-methylheterocycles.

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Supplementary files

Article information


Submitted
07 Aug 2020
Accepted
11 Oct 2020
First published
12 Oct 2020

Org. Chem. Front., 2020, Accepted Manuscript
Article type
Research Article

Selective Direct C-H Polyfluoroarylation of Electron-deficient N-heterocycle Compounds

S. Li, W. Li, X. Yang, R. Sun, J. Tang, X. Zheng, M. Yuan, R. Li, H. Chen and H. Fu, Org. Chem. Front., 2020, Accepted Manuscript , DOI: 10.1039/D0QO00923G

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