Transition Metal-Catalyzed C-H Activation/Functionalization of 8-Methylquinolines

8-Methylquinoline is regarded as an ideal substrate to participate in diversely C(sp3)-H functionalization reactions. The presence of the chelating nitrogen atom enables 8-methylquinoline to easily form cyclometallated complexes with various transition metals, leading to the selective synthesis of functionalized quinolines. Considering the great importance of quinoline cores in medicinal chemistry, in this review article, we have covered the publications related to the C-H activation and functionalization of 8-methylquinoline under transition metal catalysis during the last decade. 8-Methylquinoline is an ideal substrate for the construction of quinolin-8-ylmethanamine frameworks through C(sp3)-H functionalization. Due to the nitrogen chelating group, 8-methylquinoline can easily form cyclometallated complexes with various transition metals toward selective synthesis of functionalized quinolines. Considering the significant importance of quinoline cores in medicinal chemistry, in this review article we have covered C-H activation and functionalization of this valuable synthon under transition metal catalysis since 2014. image