4.6 Article

Highly enantioselective synthesis of Warfarin and its analogs catalysed by primary amine-phosphinamide bifunctional catalysts

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 10, Issue 40, Pages 8125-8131

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c2ob26334c

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Funding

  1. National Natural Science Foundation of China [21072020]
  2. Science and Technology Innovation Program of Beijing Institute of Technology [2011CX01008]
  3. Development Program for Distinguished Young and Middle-aged Teachers of Beijing Institute of Technology

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An efficient enantioselective Michael addition of 4-hydroxycoumarin to alpha,beta-unsaturated ketones catalysed by primary amine-phosphinamide bifunctional catalysts has been developed. This reaction afforded Warfarin and its analogs in moderate to excellent yields (up to 99%) and good to excellent enantioselectivities (up to 99% ee).

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