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

作者：Liu, Yan-Zhi; Zeng, Yao-Fu^*; Shu, Bing; Zheng, Yi-Chuan; Xiao, Lin; Chen, Shao-Yong; Song, Jia-Lin; Zhang, Xuanxuan^*; Zhang, Shang-Shi^*

来源：Organic Chemistry Frontiers, 2022, 9(16): 4287-4293.

DOI：10.1039/d2qo00763k

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

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.

• 单位
  广东药学院