C(sp[3])-H Bond Functionalization of 8-Methylquinolines.Chem Asian J. 2025 Mar 03; 20(5):e202401266.CA
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.

