Late-Stage Functionalization of Aromatic Acids with Aliphatic Aziridines: Direct Approach to Form β-Branched Arylethylamine Backbones
ACS Catalysis2019Vol. 9(8), pp. 6738–6743
Citations Over TimeTop 10% of 2019 papers
Abstract
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.
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