191673-56-0Relevant articles and documents
Asymmetric synthesis of an antagonist of neurokinin receptors: SSR 241586
Metro, Thomas-Xavier,Cochi, Anne,Gomez Pardo, Domingo,Cossy, Janine
, p. 2594 - 2602 (2011/06/20)
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
Efficient synthesis of a key intermediate of neurokinin receptor antagonists using a bifunctional asymmetric catalyst
Takamura, Makoto,Yabu, Kazuo,Nishi, Takahide,Yanagisawa, Hiroaki,Kanai, Motomu,Shibasaki, Masakatsu
, p. 353 - 356 (2007/10/03)
We report herein an efficient synthetic method for the preparation of 2-[(2R)-arylmorpholin-2-yl]ethanol, a key intermediate of neurokinin receptor antagonists. Catalytic asymmetric cyanosilylation of ketone 3 using titanium complex 4 was employed to introduce the required stereochemistry.
Heterocyclic compounds having tachykinin receptor antagonist activity their preparation and their use
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, (2008/06/13)
Compounds of the formula and quaternary ammonium ions thereof, wherein R1 and R2 are the same or different and are carbocyclic aryl or aromatic heterocyclic; A is methylene, carbonyl or sulfonyl; B is a single bond, C1-C4 alkylene or C2-C4, alkenylene; D is oxygen; E is C2 alkylene; G is C1-C4 alkylene or C2-C4 alkenylene; and L is -C(R4)(R5), wherein R4 and R5 together with the carbon atom to which they are attached represent a C5-C10 cycloalkyl or a C5-C10 heterocyclic. Especially preferred are compounds wherein L represents wherein J is a C1-C6 alkylene; Ar is a ring carbocyclic or aromatic heterocyclic and S*->O is a sulfoxide in which the sulfur atom is in the 5-configuration. The compounds have tachykinin receptor antagonist activity and exhibit an activity against both the NK1 and NK2 receptors.