4.6 Article

Scope of the organocatalysed asymmetric reductive amination of ketones with trichlorosilane

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 9, Issue 22, Pages 7860-7868

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c1ob05965c

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Funding

  1. Aesica
  2. University of Sheffield

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A highly active organocatalyst has been shown to affect the asymmetric reductive amination of ketones producing both aromatic and aliphatic amines. At 1 mol% catalyst loading, a series of structurally diverse chiral amines were quickly and economically prepared with good enantioselectivity and generally useful yield. The efficient synthesis of the calcimimetic (+)-NPS R-568 (67%, 89% ee) demonstrated the synthetic applicability of this methodology.

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