190271-58-0

Upstream product

• 909395-87-5 [(1R,2S,3S)-3-[(R)-1-(3,5-Bis-trifluoromethyl-phenyl)-ethoxy]-2-(4-fluoro-phenyl)-cyclopentyl]-carbamic acid benzyl ester 
• 849674-12-0 (1S)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl-2,2,2-trichloroethanimidoate 
• 190271-63-7 (1R,2R,3S)-3[(R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-2-(4-fluorophenyl)cyclopentane-1-carboxylic acid methyl ester 
• 405512-86-9 ((1R),(2R),(3S))-3-((1R)-1-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-2-(4-fluorophenyl)cyclopentane-carboxylic acid 
• 190269-66-0 1-[3,5-bis(trifluoromethyl)phenyl]ethyl 2,2,2-trichloroethaneimidate 
• 909395-86-4 1-{(R)-1-[(1S,2S,3R)-2-(4-Fluoro-phenyl)-3-isocyanato-cyclopentyloxy]-ethyl}-3,5-bis-trifluoromethyl-benzene 
• 68120-60-5 1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-ol 
• 30071-93-3 3,5-bis(trifluoromethyl)phenyl methyl ketone 
• 190269-78-4 (1R,2R,3S)-2-(4-fluorophenyl)-3-hydroxycyclopentane-1-carboxylic acid 

Relevant academic research and scientific papers

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.