Palladium(II)-catalyzed Oxidative C(sp3)–P Bond Formation via C(sp3)–H Bond Activation

Disclosed herein is a Pd(II)-catalyzed C(sp3)–H/P–H oxidative cross-coupling reaction between 8-methylquinolines with H-phosphonates or diarylphosphine oxides via chelation-assisted C(sp3)–H bond activation. The protocol exhibits a relatively broad functional-group tolerance and exclusive chemo- and regioselectivity. Furthermore, detailed mechanistic studies support the proposed reaction mechanism.