Enantioselective total synthesis of the oral contraceptive desogestrel by a double Heck reaction

Chemistry. 2008;14(5):1541-51. doi: 10.1002/chem.200700182.

Abstract

A novel enantioselective total synthesis of the oral contraceptive desogestrel (2) is described, in which the tetracyclic steroid core is formed by a sequence of two consecutive Heck reactions. Conversion of the known enantiopure diketone 7 led to the chiral bicycle 6 which was used for a diastereoselective intermolecular Heck reaction with vinyliodide 5 to give 15. In the following intramolecular Heck reaction, the tetracyclic ring system was formed to give 4, from which the synthesis of desogestrel (2) was furnished.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Contraceptives, Oral, Synthetic / chemical synthesis*
  • Desogestrel / chemical synthesis*
  • Hydrocarbons, Cyclic / chemistry
  • Hydrocarbons, Iodinated / chemistry
  • Ketones / chemistry
  • Models, Chemical
  • Oxidation-Reduction
  • Palladium / chemistry
  • Stereoisomerism
  • Vinyl Compounds / chemistry

Substances

  • Contraceptives, Oral, Synthetic
  • Hydrocarbons, Cyclic
  • Hydrocarbons, Iodinated
  • Ketones
  • Vinyl Compounds
  • Palladium
  • Desogestrel