Abstract Site-selective C [BOND] H borylation of quinoline derivatives at the C8 position has been achieved by using a heterogeneous Ir catalyst system based on a silica-supported cage-type monophosphane ligand SMAP. The efficient synthesis of a corticotropin-releasing factor 1 (CRF 1) receptor antagonist based on a late-stage C [BOND] H borylation strategy demonstrates the utility of the C8 borylation reaction.
