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

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.

Automated summary

In this study, a ligand-free Ir-catalyzed C-H borylation of N-acyl protected indoles was reported, providing C3 borylated indoles in good yields with excellent regioselectivities. The method was also demonstrated to be suitable for gram-scale borylation, with the C-B bonds easily converted to C-C and C-heteroatom bonds.