Solid-phase and solution-phase syntheses of oligomeric guanidines bearing peptide side chains

J Org Chem. 2005 Oct 28;70(22):8801-10. doi: 10.1021/jo051226t.

Abstract

[reaction: see text] Synthetic strategies for preparing N,N'-bridged oligomeric guanidines bearing peptide side chains both on solid support and in solution are presented. Monomers are prepared from common alpha-amino acids and therefore contain conventionally protected peptide side chains. The side chains include alkyl, aromatic, hydroxyl, amino, carboxylic acid, and amide functional groups. Oligomer elongation utilizes acid-sensitive sulfonyl activated thiourea through the formation of carbodiimide intermediate. With proper preparation of monomers, synthesis of oligomer can be performed in two directions (equivalent to N to C terminal or C to N terminal in a peptide sequence) with excellent efficiency.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Chromatography, Liquid
  • Cyclization
  • Guanidines / chemical synthesis
  • Guanidines / chemistry*
  • Mass Spectrometry
  • Molecular Structure
  • Peptides / chemistry*
  • Phase Transition
  • Solutions

Substances

  • Guanidines
  • Peptides
  • Solutions