Enantiomerically pure 2-aryl(alkyl)-2-trifluoromethylaziridines: synthesis and ring opening with selected O- and N-nucleophiles

Org Biomol Chem. 2011 Feb 21;9(4):1160-8. doi: 10.1039/c0ob00690d. Epub 2010 Dec 15.

Abstract

We report herein the synthesis of enantiomerically pure 2-phenyl- and 2-ethyl-2-trifluoromethylaziridines by Mitsunobu-type cyclisation of the corresponding N-protected amino alcohols, and our results regarding their ring opening with selected nucleophiles. Under basic conditions, N-tosyl aziridines have been regioselectively opened at the less hindered carbon. Under acidic conditions, the regioselectivity of the attack depends on the nature of the substituent at C-2 and on the nitrogen protecting group.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Aziridines / chemical synthesis*
  • Fluorine Compounds / chemical synthesis*
  • Hydrolysis
  • Models, Molecular
  • Molecular Structure
  • Stereoisomerism

Substances

  • Aziridines
  • Fluorine Compounds
  • propyleneimine