Iridium-Catalyzed Site-Selective C-H Borylation of 2-Pyridones

An iridium-catalyzed site-selective C-H borylation of 2-pyridones has been developed. The site selectivity is predominantly controlled by steric factors, and we can access C4, C5, and C6 C-H on the 2-pyridone ring by the judicious choice of ligand and solvent. Subsequent Suzuki-Miyaura cross-coupling of the borylated products also proceeds to form the corresponding arylated pyridones in good overall yields.