191673-76-4Relevant academic research and scientific papers
Salts of an optically-active sulfoxide derivative
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, (2008/06/13)
Hydrochloride of fumarate of 1-{2-[(2R)-(3,4-dichlorophenyl)-4-(3,4,5-trimethyoxybenzoyl)morpholin-2-yl]ethyl}spiro[benzo(c)thiophene-1(3H),4′-piperidin]-(2S)-oxide. These compounds have good oral adsorption and exhibit markedly excellent antagonistic act
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.
An efficient synthesis of enantiomerically pure 2-[(2R)-arylmorpholin- 2-yl]ethanols, key intermediates of tachykinin receptor antagonist
Nishi, Takahide,Ishibashi, Koki,Nakajima, Katsuyoshi,Iio, Yukiko,Fukazawa, Tetsuya
, p. 3251 - 3262 (2007/10/03)
We report herein an efficient and practical synthetic method for the preparation of enantiomerically pure 2[(2R)-arylmorpholin-2-yl]ethanols 1a- d, key intermediates of tachykinin receptor antagonist. Sharpless catalytic asymmetric dihydroxylation of 4a-d was employed to introduce the required absolute stereochemistry, and cyclization of 7a-d was accomplished by the Mitsunobu reaction.
