4.8 Article

Asymmetric Synthesis of α-Amino Ketones by Bronsted Acid Catalysis

Journal

ORGANIC LETTERS
Volume 17, Issue 15, Pages 3922-3925

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.5b01972

Keywords

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Funding

  1. NSFC [21272002, 21472150]
  2. Fundamental Research Funds for the Central Universities [XDJK2013B028]
  3. Program for New Century Excellent Talents in Universities [NCET-12-0929]

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The highly efficient, regioselective, and enantioselective transfer hydrogenation of alpha-keto ketimines and reductive amination of diketones by Bronsted acid catalysis is described. A series of chiral a-amino ketones is prepared in high yields (up to >99%), excellent regioselectivities (up to >99:1), and enantioselectivities (up to 98% ee). This method has broad substrate scope.

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