Synthesis of 13,14-secotestosterone derivatives

Steroids. 2004 Jul;69(7):501-9. doi: 10.1016/j.steroids.2004.04.010.

Abstract

A number of testosterone analogs with a 13,14-secosteroidal fragment have been prepared from (13S)-13-iodo-6beta-methoxy-3alpha, 5-cyclo-13,14-seco-5alpha-androstan-14,17-dione. The key steps involved stereoselective deiodination of the starting compound with triphenylphosphine and selective protection of the 17-keto group with trimethylsilylcyanide. Removal of iodine at C-13 proceeded with inversion of the configuration at C-13, which has been established by X-ray crystallography. 13,14-Secotestosterone analogues substituted and non-substituted at C-14 have been prepared. The obtained compounds containing flexible CD ring fragments are of great interest for comparative studies in biological tests together with testosterone and other steroids with a rigid tetracyclic skeleton.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Models, Molecular
  • Molecular Conformation
  • Secosteroids / chemical synthesis*
  • Testosterone / analogs & derivatives
  • Testosterone / chemical synthesis*

Substances

  • Secosteroids
  • Testosterone