Stereodivergent synthesis of chiral 2-alkenylaziridines: palladium(0)-catalyzed 2,3-cis-selective aziridination and base-mediated 2,3-trans-selective aziridination

Chem Pharm Bull (Tokyo). 2004 Jan;52(1):111-9. doi: 10.1248/cpb.52.111.

Abstract

Whereas treatment of the allylic mesylates of N-protected 2-alkyl-4-amino-(E)-2-alken-1-ols with sodium hydride in DMF yields exclusively the corresponding thermodynamically less stable 2,3-trans-2-alkenyl-3-alkylaziridines, exposure of the methyl carbonates of N-protected 2-alkyl-4-amino-(E)-2-alken-1-ols to a catalytic amount of Pd(PPh(3))(4) in THF or 1,4-dioxane affords predominantly the corresponding thermodynamically more stable 2,3-cis-2-alkenyl-3-alkylaziridines. The kinetically favored trans-selective aziridination would be attributed to the allylic 1,3-strain in aza-anionic intermediates. The conformational analysis of the sterically highly congested 2-alkenylaziridines thus obtained is also presented.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aziridines / chemical synthesis*
  • Aziridines / pharmacology*
  • Catalysis
  • Crystallography, X-Ray
  • Cyclization
  • Indicators and Reagents
  • Magnetic Resonance Spectroscopy
  • Models, Molecular
  • Molecular Conformation
  • Palladium / chemistry*
  • Spectrometry, Mass, Fast Atom Bombardment
  • Stereoisomerism
  • Thermodynamics

Substances

  • Aziridines
  • Indicators and Reagents
  • Palladium