On the racemization of chiral imidazolines

J Org Chem. 2008 Dec 19;73(24):9756-61. doi: 10.1021/jo8024384.

Abstract

Racemization of chiral imidazolines with base has been studied for the first time following an unexpected finding in the synthesis of chiral imidazoline ligands. Amine bases do not cause racemization. Strong inorganic bases can induce racemization, yet this occurs only when the nitrogen is unsubstituted, in agreement with a symmetry-allowed thermal disrotatory ring opening and closure from a diazapentadienyl anion. Surprisingly, even with electron-withdrawing N-substituents, no racemization is observed. Conditions which allow for the racemization-free manipulations of this important compound class have been defined and developed.

MeSH terms

  • Chromatography, High Pressure Liquid
  • Chromatography, Thin Layer
  • Dimethyl Sulfoxide
  • Imidazoles / chemical synthesis
  • Imidazoles / chemistry*
  • Isomerism
  • Ligands
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Molecular Conformation
  • Solvents
  • Stereoisomerism

Substances

  • Imidazoles
  • Ligands
  • Solvents
  • Dimethyl Sulfoxide