American Chemical Society
cs9b01347_si_002.cif (147.92 kB)

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

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posted on 2019-06-21, 00:00 authored by Kehan Zhou, Yan Zhu, Weitai Fan, Yujie Chen, Xu Xu, Jingyu Zhang, Yingsheng Zhao
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.