jo102471r_si_001.pdf (1.35 MB)

Asymmetric Synthesis of an Antagonist of Neurokinin Receptors: SSR 241586

Download (1.35 MB)
journal contribution
posted on 15.04.2011 by Thomas-Xavier Métro, Anne Cochi, Domingo Gomez Pardo, Janine Cossy
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.

History

Exports