4.8 Article

Selective Activation of Enantiotopic C(sp3)-Hydrogen by Means of Chiral Phosphoric Acid: Asymmetric Synthesis of Tetrahydroquinoline Derivatives

Journal

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 133, Issue 16, Pages 6166-6169

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ja2014955

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Funding

  1. Japan Society for the Promotion of Science
  2. Grants-in-Aid for Scientific Research [22750044, 23350046] Funding Source: KAKEN

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Chiral phosphoric acid-catalyzed asymmetric C-H functionalization has been achieved. In this process, enantiotopic C(sp(3))-hydrogen is selectively activated by chiral phosphoric acid to afford tetrahydroquinoline derivatives with excellent enantioselectivities (up to 97% ee).

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