Rhodium-Catalyzed Three-Component C(sp3)-H Activation of 8-Methyl Quinolines with Diazo Compounds and Formaldehyde/Formaldimine to Access Dual C(sp3)-C(sp3) Bonds.

The development of transition-metal-catalyzed three-component C(sp3)-H activation represents one of the most efficient strategies for the rapid construction of complex molecular architectures. Particularly, leveraging this strategy for the direct formation of dual C(sp3)-C(sp3) bonds offers distinct advantages, whereas it remains largely challenging and underdeveloped. Herein, we report a rhodium-catalyzed three-component C(sp3)-H activation of 8-methyl quinolines with diazo compounds and formaldehyde/formaldimine. This protocol not only provides a novel route for the construction of dual C(sp3)-C(sp3) bonds via a 1,1-addition process but also offers a convenient pathway to access a diverse array of 8-alkyl quinoline derivatives under mild conditions.