Late-Stage Functionalization of Aromatic Acids with Aliphatic Aziridines: A Direct Approach to Form β-Branched Arylethylamine Backbones

A palladium-catalyzed carboxylic acid-directed cross-coupling of an ortho-C(sp2) atom of aromatic acids with aliphatic aziridines to construct the β-arylethylamine skeleton via C-H activation has been developed. The reaction proceeded under mild conditions with great substrate scope. Meanwhile, the β-arylethylamine skeleton in drugs or bioactive compounds could be easily generated in a single step. A catalytic amount of cesium carbonate was crucial to realizing the selective β-arylethylamine synthesis.