4.4 Article

Synthesis of enantiopure β-amino amides via a practical reductive amination of the corresponding β-keto amides

Journal

TETRAHEDRON LETTERS
Volume 55, Issue 46, Pages 6354-6358

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2014.09.111

Keywords

beta-Keto esters; beta-Keto amides; Reductive amination; beta-Amino amides; Microwave

Funding

  1. DGRSRT (Direction Generale de la Recherche Scientifique et de la Renovation Technologique) of the Tunisian Ministry of Higher Education, Scientific Research and Technology

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A convenient and efficient reductive amination for the preparation of chiral beta-amino amides is developed utilizing microwave heating. A variety of chiral beta-keto amides react with ammonium acetate and sodium cyanoborohydride to afford the desired functionalized amines in good yields. This improved procedure takes advantage of microwave heating to significantly accelerate the reaction and offers a convenient and effective method to access some interesting molecules containing primary amine functionalities. (C) 2014 Elsevier Ltd. All rights reserved.

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