191673-45-7

Upstream product

• 95652-74-7 methyl 4-(3',4'-dichlorophenyl)-4-oxo-butanoate 
• 191673-44-6 (2R)-5-(t-butyldimethylsilyloxy)-2-(3,4-dichlorophenyl)pentane-1,2-diol 
• 191673-43-5 tert-butyl-[4-(3,4-dichloro-phenyl)-pent-4-enyloxy]-dimethyl-silane 
• 191673-42-4 methyl 4-(3,4-dichlorophenyl)-4-pentenoate 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 50597-19-8 3-(3,4-dichlorobenzoyl)-propionic acid 

Downstream Products

• 191673-46-8 (2R)-1-amino-5-(t-butyldimethylsilyloxy)-2-(3,4-dichlorophenyl)-2-pentanol 

Relevant academic research and scientific papers

Heterocyclic compounds having tachykinin receptor antagonist activity their preparation and their use

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.

Combined NK1 and NK2 tachykinin receptor antagonists: Synthesis and structure-activity relationships of novel oxazolidine analogues

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.