Easy introduction of maleimides at different positions of oligonucleotide chains for conjugation purposes

Org Biomol Chem. 2012 Nov 14;10(42):8478-83. doi: 10.1039/c2ob26514a. Epub 2012 Sep 25.

Abstract

[2,5-Dimethylfuran]-protected maleimides were placed at both internal positions and the 3'-end of oligonucleotides making use of solid-phase synthesis procedures. A new phosphoramidite derivative and a new solid support incorporating the protected maleimide moiety were prepared for this purpose. In all cases maleimide deprotection (retro-Diels-Alder reaction) followed by reaction with thiol-containing compounds afforded the target conjugate.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Furans / chemical synthesis
  • Furans / chemistry*
  • Maleimides / chemical synthesis
  • Maleimides / chemistry*
  • Oligonucleotides / chemical synthesis
  • Oligonucleotides / chemistry*
  • Organophosphorus Compounds / chemical synthesis
  • Organophosphorus Compounds / chemistry*
  • Solid-Phase Synthesis Techniques*
  • Sulfhydryl Compounds / chemical synthesis
  • Sulfhydryl Compounds / chemistry

Substances

  • Furans
  • Maleimides
  • Oligonucleotides
  • Organophosphorus Compounds
  • Sulfhydryl Compounds
  • phosphoramidite
  • maleimide
  • 2,5-dimethylfuran