Straightforward Synthesis of Purine 4'-Alkoxy-2'-deoxynucleosides: First Report of Mixed Purine-Pyrimidine 4'-Alkoxyoligodeoxynucleotides as New RNA Mimics

Org Lett. 2015 Jul 17;17(14):3426-9. doi: 10.1021/acs.orglett.5b01430. Epub 2015 Jul 2.

Abstract

Purine and pyrimidine 4'-alkoxy-2'-deoxynucleosides were efficiently prepared from nucleoside 4'-5'-enol acetates in three steps by N-iodosuccinimide promoted alkoxylation, hydrolysis, and reduction followed by conversion to phosphoramidite monomers for the solid-phase synthesis of the oligonucleotides. Fully modified 4'-alkoxyoligodeoxynucleotides, which are characterized by a prevalent N-type (RNA-like) conformation, exhibited superior chemical and nuclease resistance as well as excellent hybridization properties with a strong tendency for RNA-selective hybridization, suggesting a potential application of 4'-alkoxy-oligodeoxynucleotides in antisense technologies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Molecular Conformation
  • Molecular Structure
  • Nucleic Acid Conformation
  • Nucleic Acid Hybridization
  • Oligodeoxyribonucleotides / chemical synthesis*
  • Oligodeoxyribonucleotides / chemistry*
  • Oligonucleotides, Antisense / chemistry*
  • Purines / chemistry*
  • RNA / chemistry*
  • Succinimides / chemistry

Substances

  • Oligodeoxyribonucleotides
  • Oligonucleotides, Antisense
  • Purines
  • Succinimides
  • N-iodosuccinimide
  • RNA
  • purine