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

Abstract 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.