One-pot synthesis of optically enriched 2-piperidinones from aliphatic aldehydes and cyanoacrylamides

Org Lett. 2013 Aug 16;15(16):4054-7. doi: 10.1021/ol401951g. Epub 2013 Aug 8.

Abstract

A highly stereoselective one-pot reaction of aliphatic aldehydes and cyanoacrylamides has been developed. The one-pot reaction includes an organocatalytic Michael addition followed by an intramolecular hemiaminalization. After reduction, optically enriched 2-piperidinones with three contiguous chiral centers were obtained in up to 95% yield and 9:1 dr with 99% ee.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acrylamides / chemistry*
  • Aldehydes / chemistry*
  • Catalysis
  • Molecular Structure
  • Nitriles / chemistry*
  • Piperidones / chemical synthesis*
  • Piperidones / chemistry
  • Stereoisomerism

Substances

  • Acrylamides
  • Aldehydes
  • Nitriles
  • Piperidones
  • 2-piperidone