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 beta-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 beta-arylethylamines. The installed thiophene functional group can promote a second C-H functionalization, such as alkynylation and arylation.