Domino Knoevenagel condensation/intramolecular aldol cyclization route to diverse indolizines with densely functionalized pyridine units

J Org Chem. 2013 Oct 18;78(20):10395-404. doi: 10.1021/jo401801j. Epub 2013 Oct 8.

Abstract

A highly efficient [4 + 2] annulation route to polysubstituted indolizines is described employing a domino Knoevenagel condensation/intramolecular aldol cyclization process as a key step. Construction of pyridine rings in indolizine skeleton was rapidly achieved from several pyrrole-2-carboxaldehydes in good to excellent yields, leading to indolizines with various substituents at the 5, 6, and 7 positions depending on the reacting active methylene partners.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Cyclization
  • Indolizines / chemistry*
  • Molecular Structure
  • Pyridines / chemistry*
  • Stereoisomerism

Substances

  • Indolizines
  • Pyridines
  • indolizine