Direct Csp2-H difluoromethylation of heterocycle by K2S2O8

We reveal here a novel and efficient transition-metal-free C(sp(2))-H oxidative difluoromethylation of heterocycle. It uses stable and nontoxic NaSO2CF2H as difluoromethyl source and potassium persulfate as oxidant without the need for metal catalyst. Significantly, the reaction affords difluoromethyl heterocycles in moderate to good yields with a broad substrate tolerance. (C) 2021 Elsevier Ltd. All rights reserved.

Automated summary

An efficient transition-metal-free C(sp(2))-H oxidative difluoromethylation of heterocycle has been developed, utilizing a stable and non-toxic difluoromethyl source and oxidant. The reaction shows broad substrate tolerance and affords difluoromethyl heterocycles in moderate to good yields.