4.4 Article

1,2-Dehydrogenation of steroidal 6-methylen derivatives. Synthesis of exemestane

Journal

TETRAHEDRON
Volume 65, Issue 36, Pages 7587-7590

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2009.06.094

Keywords

Steroids; Dehydrogenation; Chloranil; Exemestane

Funding

  1. Crystal Pharma SA (Parque Tecnologico de Boecillo, Valladolid, Spain)

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The development of an efficient dehydration method of steroidal 4-en-3-ones by using chloranil and BSTFA in the presence of triflic acid in refluxing toluene allowed us, starting from testosterone, to set a large-scale procedure for the synthesis of the anti-cancer drug exemestane in 70% overall yield. (C) 2009 Elsevier Ltd. All rights reserved.

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