4.8 Article

Enantioselective Synthesis of (+)-Cortistatin A, a Potent and Selective Inhibitor of Endothelial Cell Proliferation

Journal

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 130, Issue 50, Pages 16864-+

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ja8071918

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Funding

  1. Merck Research Laboratories and Novartis
  2. Spanish MICINN

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This manuscript describes an enantioselective synthesis of the naturally occurring inhibitor of endothelial cell proliferation, cortistatin A. Key steps of the synthesis are a silicate-directed elimination/ring expansion reaction and a highly diastereoselective aza-Prins cyclization with a subsequent transannular etherification.

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