Palladium‐Catalyzed ortho‐Heteroarylation of β‐Arylethylamines Through Cross‐Dehydrogenative Coupling

A palladium‐catalyzed oxidative C–H/C–H cross‐coupling of oxalyl amide‐protected β‐arylethylamines and heteroarenes has been developed. The methodology presented a broad substrate scope, great functional group tolerance, and good to excellent yields for the synthesis of ortho‐thiophenylated β‐arylethylamines. The installed thiophene functional group can promote a second C–H functionalization, such as alkynylation and arylation. A novel and efficient oxidative C–H/C–H cross‐coupling of oxalyl amide protected β‐arylethylamines and heteroarenes by employing the palladium catalyst was reported. Various ortho‐thiophenylated β‐arylethylamines were obtained, with excellent functional group tolerance.