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Asymmetric Synthesis of an Antagonist of Neurokinin Receptors: SSR 241586

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journal contribution
posted on 15.04.2011, 00:00 authored 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.