Ring-closing metathesis-based synthesis of (3R,4R,5S)-4-acetylamino-5-amino-3-hydroxy- cyclohex-1-ene-carboxylic acid ethyl ester: a functionalized cycloalkene skeleton of GS4104

J Org Chem. 2006 Jul 7;71(14):5365-8. doi: 10.1021/jo060633h.

Abstract

(3R,4R,5S)-4-Acetylamino-5-amino-3-hydroxy-cyclohex-1-ene-carboxylic acid ethyl ester, a functionalized cyclohexene skeleton of GS4104, was diastereoselectively synthesized. A major advantage of this synthesis is the use of readily available L-serine to replace frequently used (-)-shikimic acid or (-)-quinic acid as the starting material. Ring-closing metathesis and diastereoselective Grignard reactions successfully served as the key steps. Absolute configurations of the key intermediates were confirmed by corresponding two-dimensional NMR studies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cyclization
  • Cyclohexenes / chemical synthesis*
  • Cyclohexenes / chemistry
  • Cycloparaffins / chemistry*
  • Esters / chemical synthesis*
  • Esters / chemistry
  • Molecular Conformation
  • Oseltamivir / chemistry*
  • Stereoisomerism

Substances

  • (3R,4R,5S)-4-acetylamino-5-amino-3-hydroxy- cyclohex-1-ene-carboxylic acid ethyl ester
  • Cyclohexenes
  • Cycloparaffins
  • Esters
  • Oseltamivir