Late-Stage Functionalization of Aromatic Acids with Aliphatic Aziridines: 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.

一种以钯催化为核心的羧酸导向芳酸邻位-C(sp2)原子与脂肪族氮杂环己烯的交叉偶联反应，旨在构建β-芳基乙胺骨架，并通过C-H活化实现。该反应在温和的条件下进行，具有广泛的底物适用性。同时，药物或生物活性化合物中的β-芳基乙胺骨架能够通过单步反应轻松生成。在实现选择性β-芳基乙胺合成中，催化量的碳酸铯至关重要。