Rhodium(III)-Catalyzed Site-Selective C–H Alkylation and Arylation of Pyridones Using Organoboron Reagents

In this study we developed a method for the pyridine-directed, rhodium-catalyzed, site-selective C–H alkylation and arylation of pyridones using commercially available trifluoroborate reagents. This simple and versatile transformation proceeded smoothly under relatively mild conditions with perfect site selectivity. The coupling groups in the boron reagents can be extended to primary alkyl, benzyl, and cycloalkyl. Moreover, direct C–H arylation products could also be obtained under similar conditions.