C(sp3)−H Bond Functionalization of 8‐Methylquinolines

Abstract Quinolines have emerged as essential components in various medicinal agents, playing a key role in treating various ailments. Numerous drugs with a quinoline core have been recognized for their antimalarial, antibacterial, and anticancer activities and have been successfully commercialized, including chloroquine, ciprofloxacin, topotecan, etc . Over the past two decades, a tremendous expansion in the C−H bond functionalization of quinoline scaffolds to widen this chemical space for drug discovery have been witnessed. This review article summarizes the efforts toward C(sp 3 )−H functionalization of 8‐methylquinolines for C(sp 3 )−C/X bond formation under metal and metal‐free strategies. Each section briefly overviews the C(sp 3 )−H functionalization of 8‐methylquinoline, highlighting the metal and metal‐free approaches.