Ni–Al Bimetal-Catalyzed Dual C–H Annulation of Formamides with Alkynes for Synthesis of Seven-Membered Lactams

作者：Jin Li, Yuanbin Wang, Yinpeng Wang, Yi Li, Yupeng Liu, Weiwei Xu, Mengchun Ye · 发表于：Organic Letters · 年份：2026 · DOI：10.1021/acs.orglett.6c00579 · 被引用次数：1 · 研究领域：Catalytic C–H Functionalization Methods、Cyclopropane Reaction Mechanisms、Catalytic Cross-Coupling Reactions

Seven-membered rings, prevalent in natural products, are valuable yet challenging synthetic targets. Existing strategies mainly rely on prefunctionalized substrates via dual C-FG or single C-H activation. A dual C-H annulation using non-prefunctionalized materials would offer superior atom and step economies but is daunting, as it requires sequential activation of two inert, distal C-H bonds. Herein, we report a distal 1,5-dual C-H annulation of formamides with alkynes enabled by a synergistic Ni-Al bimetallic catalyst and a tailored N-protecting group, delivering efficient access to seven-membered lactams in up to 84% yield.