191673-36-6Relevant academic research and scientific papers
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 NK1 and NK2 tachykinin receptor antagonists: Synthesis and structure-activity relationships of novel oxazolidine analogues
Nishi, Takahide,Fukazawa, Tetsuya,Ishibashi, Koki,Nakajima, Katsuyoshi,Sugioka, Yuki,Iio, Yukiko,Kurata, Hitoshi,Itoh, Kazuhiro,Mukaiyama, Osamu,Satoh, Yumiko,Yamaguchi, Takeshi
, p. 875 - 880 (2007/10/03)
We report herein the synthesis and structure-activity relationships of a series of novel oxazolidine analogues with regards to NK1 and NK2 tachykinin receptor binding affinity. Among this series of oxazolidine analogues, some compounds exhibited excellent high binding affinities for both NK1 and NK2 receptors. In addition, we describe the inhibitory effect in vivo on SP-induced airway vascular hyperpermeability and NKA-induced bronchoconstriction in guinea pigs.
