Iridium‐Catalyzed Carbonylative Synthesis of Halogen‐Containing Quinolin‐2(1H)‐ones from Internal Alkynes and Simple Anilines

Abstract

AbstractQuinolin‐2(1H)‐ones are important chemicals with various applications in pharmaceuticals. In this communication, we have developed a novel and efficient iridium‐catalyzed carbonylative annulation of simple anilines with internal alkynes for the straightforward synthesis of halogen‐containing quinolin‐2(1H)‐ones. The reaction proceeds without preactivation and directing groups through direct N–H and C–H bond activation with a broad substrate scope and high efficiency. Halogen functional groups can be well tolerated here. Remarkably, this is the first example of an iridium‐catalyzed carbonylative C–H activation of anilines.magnified image