Rhodium(iii)-catalyzed regioselective C(sp2)-H activation of indoles at the C4-position with iodonium ylides

Authors：Wu, Fuhai^*; Xiao, Lin; Xie, Hui; Chen, Shao-Yong; Song, Jia-Lin; Zheng, Yi-Chuan; Liu, Yan-Zhi; Zhang, Shang-Shi^*

Source：Organic and Biomolecular Chemistry, 2022, 20(25): 5055-5059.

DOI：10.1039/d2ob00722c

• C-H ACTIVATION
• DIRECTING GROUP
• FUNCTIONALIZATION
• ALKENYLATION
• ALKALOIDS
• CARBENES
• MILD

Herein, we report a Rh(iii)-catalyzed C4-selective activation of indoles by using iodonium ylides as carbene precursors. This protocol proceeded under redox neutral reaction conditions and provided important coupling products with good tolerance of functional groups and high yields. In addition, one-pot synthesis and scale-up and mechanistic studies were also conducted.

• Institution
  广东药学院