[4 + 2] cycloadditions of N-alkenyl iminium ions: structurally complex heterocycles from a three-component Diels-Alder reaction sequence

J Am Chem Soc. 2008 Jul 23;130(29):9222-3. doi: 10.1021/ja8028153. Epub 2008 Jun 25.

Abstract

N-Alkenyl iminium ions serve as conduits to three-component [4 + 2] cycloaddition reactions accessing structurally and stereochemically diverse piperidine derivatives. These cationic 2-azadienes participate in endo- or exo-selective [4 + 2] cycloadditions with electron-rich and neutral alkene dienophiles to generate a tetrahydropyridinium ion as the initial cycloadduct. In situ nucleophilic addition to the cycloaddition-derived iminium ion completes the three-component coupling sequence and affords a versatile synthesis of structurally complex piperidines.

Publication types

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

MeSH terms

  • Alkenes / chemistry*
  • Cyclization
  • Imines / chemistry*
  • Indoles / chemistry
  • Piperidines / chemical synthesis*

Substances

  • Alkenes
  • Imines
  • Indoles
  • Piperidines