2. Academic Validation
  3. Asymmetric synthesis of an antagonist of neurokinin receptors: SSR 241586

Asymmetric synthesis of an antagonist of neurokinin receptors: SSR 241586

  • J Org Chem. 2011 Apr 15;76(8):2594-602. doi: 10.1021/jo102471r.
Thomas-Xavier Métro 1,  Anne Cochi,  Domingo Gomez Pardo,  Janine Cossy
Affiliations

Affiliation

  • 1 Laboratoire de Chimie Organique, ESPCI ParisTech, CNRS, 10 rue Vauquelin, 75231 Paris Cedex 05, France.
PMID: 21410197 DOI: 10.1021/jo102471r
Abstract

SSR 241586 is a 2,2-disubstituted morpholine, developed by Sanofi-Aventis, which is active in the treatment of schizophrenia and irritable bowel syndrome (IBS). Different strategies have been studied to synthesize this molecule and among the strategies an organo-catalyzed Henry reaction, applied to an α-keto ester, has produced SSR 241586 in excellent enantiomeric excess.

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