Oxalyl amide assisted palladium-catalyzed arylation of C(sp2)-H bond at the δ position.

A successful protocol has been developed for δ-arylation of β-arylethamines at the ortho position under mild conditions. The newly developed methodology first presents broad substrate scope, great functional group tolerance, and good to excellent yield in the synthesis of substituted β-arylethylamines. The transformation represents a practical advantage of oxalyl amide in assistance with C-H functionalization at a remote position.