Asymmetric synthesis of tetrahydropyridines via an organocatalytic one-pot multicomponent Michael/aza-Henry/cyclization triple domino reaction

Org Lett. 2014 Nov 21;16(22):6012-5. doi: 10.1021/ol503024d. Epub 2014 Nov 7.

Abstract

A low loading of a quinine-derived squaramide efficiently catalyzes the triple-domino Michael/aza-Henry/cyclization reaction between 1,3-dicarbonyl compounds, β-nitroolefins, and aldimines to provide tetrahydropyridines bearing three contiguous stereogenic centers in good yields, excellent enantiomeric excesses, and up to high diastereomeric ratios.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Cyclization
  • Cyclobutanes / chemistry
  • Molecular Structure
  • Pyridines / chemical synthesis*
  • Pyridines / chemistry
  • Quinine / chemistry
  • Stereoisomerism
  • Sulfonamides / chemistry

Substances

  • Cyclobutanes
  • Pyridines
  • Sulfonamides
  • squaric acid amide
  • Quinine