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Practical preparation of challenging amides from non-nucleophilic amines and esters under flow conditions

机译:在流动条件下由非亲核胺和酯实际制备具有挑战性的酰胺

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摘要

A fast and efficient protocol for the formation of amides from low nucleophilic amines and esters in flow is described. Products were obtained in good to excellent yields and with the advantage of simultaneous mixing of all reagents at once, avoiding steps for intermediate formation. The protocol is also suitable to be combined with ester synthesis, resulting in the preparation of amides in-line from haloarenes.
机译:描述了一种由流动的低亲核胺和酯形成酰胺的快速有效的方法。获得的产物具有良好的产率至优异的产率,并且具有同时混合所有试剂的优势,从而避免了中间体形成的步骤。该方案也适合与酯合成结合,从而从卤代芳烃在线制备酰胺。

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  • 来源
    《Chemical Communications》 |2014年第95期|15094-15097|共4页
  • 作者单位

    University of Leuven, Department of Chemistry, Molecular Design and Synthesis, Celestijnenlaan 200F, box 2404, BE3001 Heverlee, Belgium;

    Department of Medicinal Chemistry, Janssen Research and Development, Janssen-Cilag, S.A., C/Jarama 75, 45007 Toledo, Spain;

    Department of Medicinal Chemistry, Janssen Research and Development, Janssen-Cilag, S.A., C/Jarama 75, 45007 Toledo, Spain ,Facultad de Ciencias y Tecnologias Quimicas, Universidad de Castilla-La Mancha, 13071 Ciudad Real, Spain;

    University of Leuven, Department of Chemistry, Molecular Design and Synthesis, Celestijnenlaan 200F, box 2404, BE3001 Heverlee, Belgium;

    Department of Medicinal Chemistry, Janssen Research and Development, Janssen-Cilag, S.A., C/Jarama 75, 45007 Toledo, Spain;

    Department of Medicinal Chemistry, Janssen Research and Development, Janssen-Cilag, S.A., C/Jarama 75, 45007 Toledo, Spain;

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