Asymmetric Synthesis of an Antagonist of Neurokinin Receptors: SSR 2415861

作者：Metro Thomas Xavier; Cochi Anne; Pardo Domingo Gomez^*; Cossy Janine

来源：Journal of Organic Chemistry, 2011, 76(8): 2594-2602.

DOI：10.1021/jo102471r

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 a.-keto ester, has produced SSR 241586 in excellent enantiomeric excess.

• 出版日期2011-4-15