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<p>The direct and selective C4—H functionalization of indoles remains a significant synthetic challenge. Addressing this, we disclose a highly efficient Rh(III)-catalyzed C4—H alkenylation of indoles employing <i>gem</i>-difluoromethylene alkynes. This directing group-assisted protocol delivers valuable difluorinated indole derivatives in excellent yields (up to 88%), with a broad substrate scope and exceptional functional group tolerance, providing a practical and versatile route for appealing indole diversification.</p>

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Amide-directed Rhodium(III)-catalyzed C4—H Alkenylation of Indoles with gem-Difluoromethylene Alkynes

  • 期刊论文

  • 发表日期：

    2026年3月21日

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  • Chenyu Dou,
  • Shi Cao,
  • Yahong Li,
  • Shouguo Wang

摘要

The direct and selective C4—H functionalization of indoles remains a significant synthetic challenge. Addressing this, we disclose a highly efficient Rh(III)-catalyzed C4—H alkenylation of indoles employing gem-difluoromethylene alkynes. This directing group-assisted protocol delivers valuable difluorinated indole derivatives in excellent yields (up to 88%), with a broad substrate scope and exceptional functional group tolerance, providing a practical and versatile route for appealing indole diversification.