Stereocontrolled synthesis of H-phosphonate DNA

Nucleic Acids Symp Ser (Oxf). 2006:(50):159-60. doi: 10.1093/nass/nrl079.

Abstract

Stereocontrolled synthesis of H-phosphonate DNA by an oxazaphospholidine approach is described. Diastereopure 2'-deoxynucleoside 3'-oxazaphospholidine monomers having two substituents at the 5-position of the oxazaphospholidine ring were allowed to condense with the 5'-hydroxy group of nucleosides in the presence of a less-nucleophilic acidic activator to afford the diastereopure dinucleoside phosphite intermediates. Upon treatment with an anhydrous acid, the phosphite intermediates were stereospecifically converted into the diastereopure dinucleoside H-phosphonates. The method was applied to the solid-phase synthesis of stereoregulated H-phosphonate DNA oligomers containing four kinds of nucleobases.

MeSH terms

  • DNA / chemistry
  • Deoxyribonucleosides / chemistry
  • Oligodeoxyribonucleotides / chemical synthesis*
  • Oligodeoxyribonucleotides / chemistry
  • Organophosphonates / chemistry
  • Stereoisomerism

Substances

  • Deoxyribonucleosides
  • Oligodeoxyribonucleotides
  • Organophosphonates
  • DNA