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<p>The development of robust, practical, and chemoselective methods for introducing the difluoromethyl (CF₂H) group into organic molecules is highly sought after in the fields of pharmaceutical and agrochemical design. Herein, we report a Fe/Ni dual-transition-metal electrocatalytic strategy for difluoromethylation of (hetero)aryl halides, using difluoroacetate—the most abundant source of the CF₂H group—as an effective difluoromethylating reagent. A diverse array of aryl and heteroaryl halides, bearing synthetically useful functional groups, can be readily converted into the corresponding difluoromethylated products with good efficiency. This difluoromethylation protocol is readily scalable and is successfully applied to the preparation and late-stage functionalization of bioactive molecules.</p>

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Dual transition metal electrocatalysis for difluoromethylation of Aryl halides using potassium difluoroacetate

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年11月28日

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  • Naifu Zhou,
  • Mingding Chai,
  • Niankai Fu

摘要

The development of robust, practical, and chemoselective methods for introducing the difluoromethyl (CF₂H) group into organic molecules is highly sought after in the fields of pharmaceutical and agrochemical design. Herein, we report a Fe/Ni dual-transition-metal electrocatalytic strategy for difluoromethylation of (hetero)aryl halides, using difluoroacetate—the most abundant source of the CF₂H group—as an effective difluoromethylating reagent. A diverse array of aryl and heteroaryl halides, bearing synthetically useful functional groups, can be readily converted into the corresponding difluoromethylated products with good efficiency. This difluoromethylation protocol is readily scalable and is successfully applied to the preparation and late-stage functionalization of bioactive molecules.