Remote C−H Functionalization of 8‐Aminoquinolinamides

Abstract

Abstract8‐Aminoquinoline, a common structural motif present in many natural products, pharmaceuticals, agrochemicals, and important drugs has always been an attractive scaffold in synthetic organic chemistry. Recent years have witnessed the development of 8‐aminoquinoline as a ligand in transition‐metal‐catalyzed C−H functionalizations. Therefore, synthesis of functionalized 8‐aminoquinolines is of great importance and rapid generation of functionalized quinolines could be achieved by direct C−H functionalization. In this regard, since the seminal report of distal C5‐H halogenations of quinoline, diverse C−X bond formation reactions have been published. This review is focused on the C5‐H functionalization of 8‐aminoquinolinamide derivatives, including not only C−C bond formation reactions but also carbon–heteroatom bond formations such as C−X (X=F, Cl, Br, I) C−S, C−Se, C−N, C−O, and C−P. In most cases, the C5 position is activated by a single electron transfer method employing either metal catalysts, photocatalysts, or metal‐free conditions.