BH3-promoted stereoselective β-lithiation of N-alkyl-2-phenylaziridines

J Org Chem. 2011 Apr 1;76(7):2291-5. doi: 10.1021/jo102474u. Epub 2011 Mar 2.

Abstract

BH(3) complexes of N-alkyl-2-phenylaziridines have been synthesized and their structure and stereochemistry proved with DFT calculations and NMR experiments. It has been demonstrated that the Lewis acid complexation is able to promote a regioselective β-lithiation in 2-phenylaziridino-borane complexes. The lithiated intermediates were configurationally stable, allowing an enantioselective preparation of cis-2,3-disubstituted aziridines.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkanes / chemistry*
  • Aziridines / chemistry*
  • Boranes / chemistry*
  • Lithium / chemistry*
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Stereoisomerism

Substances

  • Alkanes
  • Aziridines
  • Boranes
  • Lithium