Rhodium(III)-catalyzed C(sp3)-H Amidation of 8-Methylquinolines with Amides at Room Temperature

Here we disclose a Rh(III)-catalyzed chelation-assisted C(sp(3))-H activation of 8-methylquinolines, which can enable intermolecular amidation using commercially available, reliable amides as the amidating reagent to provide an efficient route to quinolin-8-ylmethanamine derivatives. This amidation proceeds at room temperature in moderate to excellent yields, and features good functional group tolerance and complete mono-selectivity.