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Asymmetric Synthesis of an Antagonist of Neurokinin Receptors: SSR 241586
Author(s) -
ThomasXavier Métro,
Anne Cochi,
Domingo Gomez Pardo,
Janine Cossy
Publication year - 2011
Publication title -
the journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.2
H-Index - 228
eISSN - 1520-6904
pISSN - 0022-3263
DOI - 10.1021/jo102471r
Subject(s) - neurokinin b , tachykinin receptor , substance p , neurokinin a , bronchoconstriction , nk1 receptor antagonist , chemistry , antagonist , receptor , neurogenic inflammation , pharmacology , neuropeptide , irritable bowel syndrome , medicine , asthma , biochemistry
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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