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.

本研究开发了一种以羧酸为导向基团的钯催化交叉偶联反应：通过C-H活化，实现芳香羧酸邻位C(sp²)原子与脂肪族氮丙啶的偶联，进而构建β-芳基乙胺骨架。该反应可在温和条件下进行，且底物适用范围广泛。同时，该方法可通过一步反应便捷地制备药物或生物活性分子中的β-芳基乙胺骨架。催化量的碳酸铯是实现该选择性β-芳基乙胺合成的关键因素。