Tetrahedron

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

A Marcos-Escribano, FA Bermejo, AL Bonde-Larsen…

Index: Marcos-Escribano, Andres; Bermejo, Francisco A.; Bonde-Larsen, Antonio Lorente; Retuerto, Jesus Iglesias; Sierra, Ignacio Herraiz Tetrahedron, 2009 , vol. 65, # 36 p. 7587 - 7590

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Citation Number: 8

Abstract

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.