1579952-92-3

Upstream product

• 1579952-91-2 C₂₇H₂₈FNO₃ 
• 618386-44-0 C₂₈H₃₀FNO₃ 
• 618386-13-3 C₂₆H₂₆FNO₃ 
• 618386-45-1 (3R,3aS,4S,4aR,7R,8aS,9aR)-4-((E)-2-(5-(3-fluorophenyl)pyridin-2-yl)vinyl)-7-(hydroxymethyl)-3-methyldecahydronaphtho[2,3-c]furan-1(3H)-one 
• 3019-71-4 Trichloroacetyl isocyanate 

Downstream Products

• 1579952-93-4 (1R,3aR,4aR,4'S,8aR,9S,9aS)-9-((E)-2-(5-(3-fluorophenyl)pyridin-2-yl)vinyl)-1-methyloctahydro-1H-spiro[naphtho[2,3-c]furan-6,4'-oxazolidine]-2',3(7H)-dione 

Relevant academic research and scientific papers

Himbacine-derived thrombin receptor antagonists: C7-Spirocyclic analogues of vorapaxar

We have synthesized several C7-spirocyclic analogues of vorapaxar and evaluated their in vitro activities against PAR-1 receptor. Some of these analogues showed activities and rat plasma levels comparable to vorapaxar. Compound 5c from this series showed excellent PAR-1 activity (K i = 5.1 nM). We also present a model of these spirocyclic compounds docked to the PAR-1 receptor based on the X-ray crystal structure of vorapaxar bound to PAR-1 receptor. This model explains some of the structure-activity relationships in this series.