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.
Combined tachykinin receptor antagonist: Synthesis and stereochemical structure-activity relationships of novel morpholine analogues
Nishi, Takahide,Ishibashi, Koki,Takemoto, Toshiyasu,Nakajima, Katsuyoshi,Fukazawa, Tetsuya,Iio, Yukiko,Itoh, Kazuhiro,Mukaiyama, Osamu,Yamaguchi, Takeshi
, p. 1665 - 1668 (2007/10/03)
We report herein the synthesis and stereochemical structure-activity relationships of novel morpholine analogues 12 and 13 with regards to NK1, NK2 and NK3 tachykinin receptor binding affinity. An essential requirement for more potent binding affinities was controlled by absolute configuration. (S,R)-12 and (S,R)-13 exhibited high binding affinities for NK1, NK2 and NK3 receptors. (C) 2000 Elsevier Science Ltd. All rights reserved.
