4.8 Article

Enantioselective Synthesis of (+)-Cephalostatin 1

Journal

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 132, Issue 1, Pages 275-280

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ja906996c

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Funding

  1. Novartis
  2. Taiho Pharmaceutical Co., Ltd.

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This Article describes an enantioselective synthesis of cephalostatin 1. Key steps of this synthesis are a unique methyl group selective allylic oxidation, directed C-H hydroxylation of a sterol at C12, Au(I)-catalyzed 5-endo-dig cyclization, and a kinetic spiroketalization.

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