Flexible, phase-transfer catalyzed approaches to 4-substituted prolines

Org Lett. 2014 Sep 19;16(18):4778-81. doi: 10.1021/ol502239g. Epub 2014 Sep 5.

Abstract

A range of 4-substituted prolines can be rapidly synthesized from a protected glycine Schiff base in only four steps and in 27-55% overall yield. Phase transfer catalysis allows direct access to both enantiomeric series, and the relative stereochemistry at the 4-position is readily controlled (>10:1 dr) through the choice of hydrogenation conditions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Catalysis
  • Glycine / chemistry*
  • Hydrogenation
  • Molecular Structure
  • Oligopeptides / pharmacology
  • Proline / analogs & derivatives*
  • Proline / chemical synthesis*
  • Proline / chemistry
  • Schiff Bases
  • Stereoisomerism

Substances

  • Oligopeptides
  • Schiff Bases
  • bisebromoamide
  • Proline
  • Glycine