Aminocarbonylation of 4-iodo-1H-imidazoles with an amino acid amide nucleophile: synthesis of constrained H-Phe-Phe-NH2 analogues

J Org Chem. 2013 Dec 6;78(23):12251-6. doi: 10.1021/jo4020613. Epub 2013 Nov 14.

Abstract

A simple and an expedient process to prepare 5-aryl-1-benzyl-1H-imidazole-4-carboxamides by the aminocarbonylation of 5-aryl-4-iodo-1H-imidazoles using ex situ generation of CO from Mo(CO)6 with an amino acid amide nucleophile is reported. Furthermore, a microwave-assisted protocol for the direct C-5 arylation of 1-benzyl-1H-imidazole and a regioselective C-4 iodination method to acquire starting material for our aminocarbonylation are presented. The method can be used to prepare imidazole based peptidomimetics, herein exemplified by the synthesis of constrained H-Phe-Phe-NH2 analogues.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemistry*
  • Amino Acids / chemistry*
  • Imidazoles / chemistry*
  • Molecular Structure
  • Peptide Fragments / chemical synthesis*
  • Peptide Fragments / chemistry

Substances

  • Amides
  • Amino Acids
  • Imidazoles
  • Peptide Fragments