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Copper-Catalyzed Annulative Amination of ortho-Alkynylphenols with Hydroxylamines: Synthesis of 3-Aminobenzofurans by Umpolung Amination Strategy

Koji Hirano*, Tetsuya Satoh and Masahiro Miura*

*Department of Applied Chemistry, Faculty of Engineering, Osaka University, Suita, Osaka 565-0871, Japan, Email:,

K. Hirano, T. Satoh, M. Miura, Org. Lett., 2011, 13, 2395-2397.

DOI: 10.1021/ol200651r (free Supporting Information)

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A room temperature copper-catalyzed annulative amination of ortho-alkynylphenols with O-acylated hydroxylamines as electrophilic amination reagents proceeds efficiently to provide the corresponding 3-aminobenzofurans of biological and pharmaceutical interest.

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ID: J54-Y2011-1390