Palladium-Catalyzed Regioselective C-H Arylation of Quinoline-N-Oxides at C-8 Position using Diaryliodonium Salts

A simple and efficient Pd(II)-catalyzed site-selective direct arylation strategy was demonstrated for the synthesis of 8-arylquinoline-N-oxide derivatives using quinoline-N-oxides and (aryl)(mesityl)iodonium triflates. A series of control experiments were carried out to elucidate the reaction mechanism. The synthetic potential was extended with the C-2 post-modification of the final derivative.