Selective direct C–H polyfluoroarylation of electron-deficient N-heterocyclic compounds

Abstract

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