Conception and evolution of stereocontrolled strategies toward functionalized 8-aryloctanoic acids related to the total synthesis of aliskiren

J Org Chem. 2014 Oct 17;79(20):9531-45. doi: 10.1021/jo5015195. Epub 2014 Oct 6.

Abstract

A detailed account is given describing the approaches used toward the total synthesis of aliskiren. In particular, ring-closing metathesis with the Hoveyda-Grubbs catalyst accelerates the formation of a 9-membered lactone from an (R)-ester. The diastereomeric (S)-ester leads to the formation of dimeric dilactones, which were characterized by X-ray analysis and chemical conversions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis*
  • Amides / chemistry
  • Caprylates / chemistry*
  • Catalysis
  • Crystallography, X-Ray
  • Esters
  • Fumarates / chemical synthesis*
  • Fumarates / chemistry
  • Lactones / chemistry*
  • Molecular Structure
  • Stereoisomerism

Substances

  • Amides
  • Caprylates
  • Esters
  • Fumarates
  • Lactones
  • aliskiren