Fully automated synthesis of DNA-binding Py-Im polyamides using a triphosgene coupling strategy

Org Lett. 2015 Jan 2;17(1):158-61. doi: 10.1021/ol503388a. Epub 2014 Dec 12.

Abstract

The fully automated solid-phase synthetic strategy of hairpin pyrrole-imidazole polyamides is described. A key advance is the development of methodology for the application of triphosgene as a coupling agent in the automated synthesis of hairpin polyamides without racemization. This automated methodology is compatible with all the typical building blocks, enabling the facile synthesis of polyamide libraries in good yield (9-15%) and crude purity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Combinatorial Chemistry Techniques
  • DNA / chemistry*
  • Imidazoles / chemical synthesis*
  • Imidazoles / chemistry
  • Molecular Structure
  • Nylons / chemical synthesis*
  • Nylons / chemistry
  • Pyrroles / chemical synthesis*
  • Pyrroles / chemistry
  • Solid-Phase Synthesis Techniques

Substances

  • Imidazoles
  • Nylons
  • Pyrroles
  • DNA