Urea-accelerated Iridium-catalyzed 2-Position-selective C–H Borylation of Indole Derivatives

We developed iridium-catalyzed 2-position-selective C–H borylation of indole derivatives by modifying the structure a bipyridine-type ligand. The yields ranged from good to excellent, even on gram scale, and were dramatically improved addition urea derivative catalyst. introduced boryl group was converted chloro, bromo, phenyl groups without isolation borylated intermediate. Preliminary results indicated importance hydrogen bonding between substrate additive.