Chelating Group Enabled Palladium‐Catalyzed Regiodivergent Carbonylative Synthesis of 2,3‐Dihydroquinolin‐4(1 H )‐ones

A new procedure on palladium‐catalyzed carbonylative cyclization of N‐ (2‐pyridyl)sulfonyl ( N ‐SO 2 Py)‐2‐iodoanilines with terminal alkenes has been developed for the rapid construction of dihydroquinolin‐4(1 H )‐one scaffolds. Enabled by the chelating group and using benzene‐1,3,5‐triyl triformate (TFBen) as the CO source, both aromatic and aliphatic alkenes were smoothly transformed into the corresponding 2,3‐dihydroquinolin‐4(1 H )‐ones in good yields with excellent regioselectivities. Notably, the reaction of aromatic alkenes produces 2‐aryl‐2,3‐dihydroquinolin‐4(1 H )‐ones, while 3‐alkyl‐2,3‐dihydroquinolin‐4(1 H )‐ones were obtained when aliphatic alkenes were used. This protocol has been applied in the synthesis of antitumor agent A as well.