Organocatalyzed Protecting-Group-Free Total Synthesis of (S,S)- and (S,R)-Reboxetine, an Antidepressant Drug

J Org Chem. 2022 Aug 5;87(15):10430-10434. doi: 10.1021/acs.joc.2c00886. Epub 2022 Jul 22.

Abstract

An efficient, simple, and concise organocatalyzed protecting-group-free synthetic approach to the stereoisomers of the antidepressant drug reboxetine and its implementation toward the asymmetric synthesis of (S,S)-reboxetine and (S,R)-reboxetine from commercially available trans-cinnamaldehyde are described. The synthesis features organocatalytic Jørgensen asymmetric epoxidation, epoxide migration, and Mitsunobu inversion as key steps.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antidepressive Agents*
  • Morpholines*
  • Reboxetine
  • Stereoisomerism

Substances

  • Antidepressive Agents
  • Morpholines
  • Reboxetine