A Highly Active Palladium System Catalyzed C2‐Arylation of N‐Acyl Pyrroles with Aryl Halides and Their Biological Activity

Abstract The formation of C−C bonds is a fundamental bond construction in organic synthesis. In this study, a highly active palladium catalytic system has been developed for the C2‐arylation of N ‐acyl pyrroles with aryl halides in the help of copper additive and K 2 CO 3 . The reactions proceed smoothly under mild conditions and have excellent functional group compatibility. Especially, this protocol provides a straightforward method for the utilization of aryl chlorides in coupling reactions. A variety of valuable arylated N ‐acyl pyrroles were synthesized and found to exhibit certain anti‐inflammatory activity.