Copper‐Catalyzed N‐Arylation with Boronic Acid Pinacol Esters

Abstract A copper‐catalyzed facile N‐arylation of 2‐acyl substituted anilines has been disclosed. Through chelation assistance of the weakly coordinating carbonyl groups, the Chan−Evans−Lam (CEL) C−N cross‐coupling reactions proceeded at room temperature in open flasks. Furthermore, such chelation effects also enabled the direct utilization of aryl boronic acid pinacol esters in Cu‐catalyzed CEL reactions under mild conditions.