190271-63-7

Upstream product

• 912807-23-9 (1R,2R,3S)-2-(4-Fluoro-phenyl)-3-trimethylsilanyloxy-cyclopentanecarboxylic acid methyl ester 
• 30071-93-3 3,5-bis(trifluoromethyl)phenyl methyl ketone 
• 68120-60-5 1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-ol 
• 405512-86-9 ((1R),(2R),(3S))-3-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-2-(4-fluorophenyl)cyclopentane-carboxylic acid 
• 18107-18-1 diazomethyl-trimethyl-silane 
• 459174-07-3 (S)-(-)-methyl 2-(4-fluorophenyl)-3-hydroxycyclopent-1-enecarboxylate 
• 379679-70-6 2-(4-fluorophenyl)-1,3-cyclopentanedione 
• 379679-64-8 methyl 2-(4-fluorophenyl)-3-oxo-1-cyclopent-1-enecarboxylate 
• 379679-62-6 3-bromo-2-(4-fluorophenyl)-2-cyclopenten-1-one 
• 368-63-8 (R)-[3,5-bis(trifluoromethyl)phenyl]ethanol 
• 352-33-0 1-Chloro-4-fluorobenzene 
• 3859-41-4 1,3-cyclopentadione 
• 190269-75-1 methyl (1R,2R,3S)-2-(4-fluorophenyl)-3-hydroxycyclopentane-1-carboxylate 
• 225920-05-8 (S)-3,5-bis(trifluoromethyl)-1-phenylethanol 

Downstream Products

• 405512-86-9 ((1R),(2R),(3S))-3-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-2-(4-fluorophenyl)cyclopentane-carboxylic acid 
• 1007593-13-6 C₂₃H₂₀ClF₇O₂ 
• 405512-89-2 ((1R),(2R),(3S))-3-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-2-(4-fluorophenyl)cyclopentanecarboxaldehyde 
• 190266-45-6 [(1R,2R,3S)-3-{(R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy}-2-(4-fluorophenyl)cyclopentyl]methanol 
• 909396-01-6 [(1R,2S,3S)-3-[(R)-1-(3,5-Bis-trifluoromethyl-phenyl)-ethoxy]-2-(4-fluoro-phenyl)-cyclopentyl]-(2-methoxy-ethyl)-carbamic acid benzyl ester 
• 909396-00-5 [(1R,2S,3S)-3-[(R)-1-(3,5-Bis-trifluoromethyl-phenyl)-ethoxy]-2-(4-fluoro-phenyl)-cyclopentyl]-ethyl-carbamic acid benzyl ester 

Relevant academic research and scientific papers

PROCESS FOR MAKING LACTAM TACHYKININ RECEPTOR ANTAGONISTS

The present invention is directed to a process for preparing certain α,α disubstituted γ-lactam derivatives that are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful i

COMBINATION THERAPY FOR THE TREATMENT OF URINARY FREQUENCY, URINARY URGENCY AND URINARY INCONTINENCE

This invention concerns compositions for the treatment of urinary frequency, urinary urgency and urinary incontinence comprising a selected antagonist of the NK-1 receptor or a pharmaceutically acceptable salt thereof and an anti-muscarinic agent or a pha

Stereoselective preparation of a cyclopentane-based NK1 receptor antagonist bearing an unsymmetrically substituted sec-sec ether

A highly efficient synthesis of the potent and selective NK-1 receptor antagonist 1 is described. The key transformation involved the etherification reaction between cyclopentanol 12 and chiral imidate 30 which was catalyzed by HBF4 to initially give ether 14 as a 17:1 mixture of diastereomers and in 75% combined yield. The diastereoselectivity was upgraded to 109:1 by crystallization of the triethylamine solvate 44 which was isolated in 54% yield from 12. Mechanistic studies confirmed that the etherification reaction proceeds through an unprecedented SN2 reaction pathway under typical S N1 reaction conditions.

Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives

The synthesis and optimization of a cyclopentane-based hNK1 antagonist scaffold 3, having four chiral centers, will be discussed in the context of its enhanced water solubility properties relative to the marketed anti-emetic hNK1 antagonist EMEND (Aprepitant). Sub-nanomolar hNK1 binding was achieved and oral activity comparable to Aprepitant in two in vivo models will be described.

Lactam tachykinin receptor antagonists

The present invention is directed to certain lactam compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations compri