Stereoselective synthesis of amido and phenyl azabicyclic derivatives via a tandem aza Prins-Ritter/Friedel-Crafts type reaction of endocyclic N-acyliminium ions

J Org Chem. 2013 Nov 1;78(21):10629-41. doi: 10.1021/jo401450j. Epub 2013 Oct 14.

Abstract

A simple protocol is described for the synthesis of amido and phenyl hexahydroindolizin-3(2H)-one, hexahydro-1H-quinolizin-4(6H)-one, and 1,3,4,10b-tetrahydropyrido[2,1-a]isoindol-6(2H)-one derivatives via endo-trig (aza-Prins type) cyclization followed by an intermolecular Ritter/Friedel-Crafts reaction of cyclic N-acyliminium ions, which are derived from the boron trifluoride etherate treatment of regioselectively reduced N-homoallyl imides. The reactions are highly diastereoselective with excellent yields.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis*
  • Amides / chemistry
  • Azabicyclo Compounds / chemical synthesis*
  • Azabicyclo Compounds / chemistry
  • Indolizines / chemistry*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Amides
  • Azabicyclo Compounds
  • Indolizines