Synthetic approaches to a chiral 4-amino-3-hydroxy piperidine with pharmaceutical relevance

Org Biomol Chem. 2012 Jul 21;10(27):5253-7. doi: 10.1039/c2ob25411e. Epub 2012 May 31.

Abstract

Four synthetic strategies were evaluated towards the preparation of (-)-(3R,4R)-1-benzyl-4-(benzylamino)piperidin-3-ol (1), which was constructed with control over the relative and absolute stereochemistry of the 4,3-amino alcohol moiety. The first strategy employed a novel Rh(I) catalyzed asymmetric hydrogenation, while two other strategies exploited the existing stereochemistry in 2-deoxy-D-ribose, and the fourth explored both biocatalytic and classical resolution techniques as a means to impart enantioenrichment to racemic intermediates en route to targeted structure (-)-1.

MeSH terms

  • Hydrogenation
  • Models, Molecular
  • Molecular Structure
  • Piperidines / chemical synthesis*
  • Stereoisomerism

Substances

  • Piperidines