Unstabilized azomethine ylides for the stereoselective synthesis of substituted piperidines, tropanes, and azabicyclo[3.1.0] systems

J Am Chem Soc. 2013 Feb 20;135(7):2478-81. doi: 10.1021/ja312311k. Epub 2013 Feb 11.

Abstract

Acid treatment of densely substituted 2-silyl-1,2-dihydropyridines provides a new and convenient entry to reactive azomethine ylides that can (1) be protonated and reduced with high stereoselectivity to give piperidines, (2) participate in [3 + 2] dipolar cycloaddition to give tropanes, and (3) undergo a Nazarov-like 6-π electrocyclization that upon reduction give 2-azabicyclo[3.1.0] systems.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Aza Compounds / chemical synthesis*
  • Aza Compounds / chemistry
  • Azo Compounds / chemistry*
  • Bridged Bicyclo Compounds / chemical synthesis*
  • Bridged Bicyclo Compounds / chemistry
  • Cyclization
  • Magnetic Resonance Spectroscopy
  • Piperidines / chemical synthesis*
  • Piperidines / chemistry
  • Stereoisomerism
  • Thiosemicarbazones / chemistry*
  • Tropanes / chemical synthesis*
  • Tropanes / chemistry

Substances

  • Aza Compounds
  • Azo Compounds
  • Bridged Bicyclo Compounds
  • Piperidines
  • Thiosemicarbazones
  • Tropanes
  • azomethine