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Rh(iii)-Catalyzed dienylation and cyclopropylation of indoles at the C4 position with alkylidenecyclopropanes

Liu, Yan-Zhi; Zeng, Yao-Fu*; Shu, Bing; Zheng, Yi-Chuan; Xiao, Lin; Chen, Shao-Yong; Song, Jia-Lin; Zhang, Xuanxuan*; Zhang, Shang-Shi*
Science Citation Index Expanded
广东药学院

摘要

Herein, we report a Rh(iii)-catalyzed C-H functionalization of indoles at the C4 position with alkylidenecyclopropanes (ACPs). Motifs of dienes or cyclopropanes could be selectively introduced into indoles by choosing different ACPs. This protocol displayed excellent regioselectivity and broad substrate scope. A scale-up experiment and mechanistic studies were also performed.

关键词

H ACTIVATION CATALYZED HYDROARYLATIONS DIRECTING GROUP METHYLENECYCLOPROPANES FUNCTIONALIZATION BENZANNULATION ALKENYLATION HETEROCYCLES ALKYLATION ANNULATION