Ligand-free iridium-catalyzed regioselective C-H borylation of indoles

Zilong Pan; Luhua Liu; Senmiao Xu; Zhenlu Shen

doi:10.1039/d0ra10211c

Ligand-free iridium-catalyzed regioselective C-H borylation of indoles

RSC Adv. 2021 Jan 29;11(10):5487-5490. doi: 10.1039/d0ra10211c. eCollection 2021 Jan 28.

Authors

Zilong Pan^{1

2

3}, Luhua Liu^{2

3}, Senmiao Xu², Zhenlu Shen¹

Affiliations

¹ College of Chemical Engineering, Zhejiang University of Technology Hangzhou 310014 China zhenlushen@zjut.edu.cn.
² State Key Laboratory for Oxo Synthesis and Selective Oxidation, Center for Excellence in Molecular Science, Suzhou Research Institute, Lanzhou Institute of Chemical Physics, Chinese Academy of Science Lanzhou 730000 China senmiaoxu@licp.cas.cn.
³ University of Chinese Academy of Sciences Beijing 100049 China.

Abstract

We herein report a ligand-free Ir-catalyzed C-H borylation of N-acyl protected indoles. This simple protocol could tolerate a variety of functional groups, affording C3 borylated indoles in good yields with excellent regioselectivities. We also demonstrated that the current method is amenable to gram-scale borylation and the C-B bonds could be easily converted to C-C and C-heteroatom bonds.