Synthesis of side-chain homologated analogs of 1,25-dihydroxycholecalciferol and 1,25-dihydroxyergocalciferol

Steroids. 1991 Jun;56(6):311-5. doi: 10.1016/0039-128x(91)90052-w.

Abstract

A novel synthesis of side-chain homologated analogs of vitamin D isomers has been described. The synthesis allows for the insertion of the double bond into the C-24 position of the side chain. The key synthetic step involves the coupling of a new C24-vitamin D synthon with the respective side-chain fragment. The method is illustrated by the preparation of (24E)-24,24a-dehydro-24,24-dihomo-1,25-dihydroxycholecalcife rol (1) and (24b R)- and (24b S)-24,24-dihomo-1,25-dihydroxyergocalciferols (2 and 3). Trans geometry of the newly formed double bond in the side chain was confirmed by high field nuclear magnetic resonance spectra.

MeSH terms

  • Calcitriol / analogs & derivatives*
  • Calcitriol / chemical synthesis
  • Calcitriol / chemistry
  • Ergocalciferols / chemical synthesis*
  • Ergocalciferols / chemistry
  • Magnetic Resonance Spectroscopy
  • Molecular Structure

Substances

  • Ergocalciferols
  • 1,25-dihydroxyergocalciferol
  • Calcitriol