Direct entry to peptidyl ketones via SmI2-mediated C-C bond formation with readily accessible N-peptidyl oxazolidinones

J Org Chem. 2008 Feb 1;73(3):1088-92. doi: 10.1021/jo702286b. Epub 2007 Dec 29.

Abstract

In this work, a new method for the preparation of peptidyl ketones is presented employing a SmI(2)/H(2)O-mediated coupling of N-peptidyl oxazolidinones with electron-deficient alkenes. The requisite peptide imides were easily prepared by solution-phase peptide synthesis starting from an N-acyl oxazolidinone derivative of an amino acid. Importantly, they could be used directly in the C-C bond-forming step without the need for further functionalization. Coupling of these peptide derivatives with a second peptide possessing an N-terminal acryloyl group leads to ketomethylene isosteres of glycine-containing peptides. This method represents an alternative means for ligating two small peptides through a C-C bond-forming step.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylamides / chemistry
  • Amines / chemistry
  • Amino Acids / chemistry
  • Carbon / chemistry*
  • Free Radicals / chemistry
  • Iodides / chemistry*
  • Ketones / chemical synthesis*
  • Ketones / chemistry
  • Molecular Structure
  • Oxazolidinones / chemistry*
  • Peptides / chemistry*
  • Samarium / chemistry*

Substances

  • Acrylamides
  • Amines
  • Amino Acids
  • Free Radicals
  • Iodides
  • Ketones
  • Oxazolidinones
  • Peptides
  • Samarium
  • Carbon
  • samarium diiodide
  • tert-butylacrylamide