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 pathway.