Palladium-catalyzed oxalyl amide assisted direct ortho-alkynylation of arylalkylamine derivatives at δ and ε positions

Palladium-catalyzed oxalyl amide directed ortho-alkynylation of arylalkylamine derivatives is reported for the first time. A wide variety of beta-arylethamine and gamma-arylpropamine derivatives are compatible with this protocol. This method provides a general means to synthesize substituted alkynylarylalkylamine derivatives, highlighting the ability of oxalyl amide in promoting C-H functionalization at unique delta and epsilon positions.