American Chemical Society
ol0c01183_si_001.pdf (7.82 MB)

Palladium-Catalyzed Cascade Decarboxylative Amination/6-endo-dig Benzannulation of o‑Alkynylarylketones with N‑Hydroxyamides To Access Diverse 1‑Naphthylamine Derivatives

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journal contribution
posted on 2020-05-04, 11:35 authored by Youpeng Zuo, Xinwei He, Qiang Tang, Wangcheng Hu, Tongtong Zhou, Yongjia Shang
An efficient and practical one-pot strategy to produce highly substituted 1-naphthylamines via sequential palladium-catalyzed decarboxylative amination/intramolecular 6-endo-dig benzannulation reactions has been described. In this reaction, a broad range of electron-rich, electron-neutral, and electron-deficient o-alkynylarylketones react well with N-hydroxyl aryl/alkylamides to give a diversity of 1-naphthylamines in good to excellent yields under mild reaction conditions. The gram-scale synthesis, with benefits such as undiminished product yield and easy transformation, illustrated the practicality of this method.