Further studies on the synthesis of 24(S),25-epoxycholesterol. A new, efficient preparation of desmosterol

J Org Chem. 2000 Apr 7;65(7):1919-23. doi: 10.1021/jo991370c.

Abstract

Efforts to improve the synthesis of 24(S),25-epoxycholesterol (1) from stigmasterol (3) have included identification of 6 alpha-hydroxy-i-steroid 11 as a byproduct from the ozonolysis of 9 and an attempt to effect conversion of sulfone 14 to diol 18 via Payne rearrangement and nucleophilic trapping of epoxide 25, which led instead to 27 and 28 (97% yield). A more efficient synthesis of 1 was achieved via coupling of cuprate 21 with allylic acetate 31 to give 73% of 16, in the most efficient conversion yet of a C22 intermediate to desmosterol (5) or its acetate 6.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Catalysis
  • Cholesterol / analogs & derivatives*
  • Cholesterol / chemical synthesis
  • Desmosterol / chemical synthesis*
  • Magnetic Resonance Spectroscopy

Substances

  • Desmosterol
  • 24,25-epoxycholesterol
  • Cholesterol