1579952-83-2

Upstream product

• 1579952-82-1 C₂₈H₃₀F₃NO₃ 
• 3019-71-4 Trichloroacetyl isocyanate 
• 1579952-81-0 (3R,3aS,4S,4aR,8aR,9aR)-3-methyl-7-methylene-4-((E)-2-(5-(3-(trifluoromethyl)phenyl)pyridin-2-yl)vinyl)decahydronaphtho[2,3-c]furan-1(3H)-one 

Downstream Products

• 1579952-90-1 3-(6-((E)-2-((1R,3aR,4aR,4'R,8aR,9S,9aS)-1-methyl-2',3-dioxodecahydro-1H-spiro[naphtho[2,3-c]furan-6,4'-oxazolidin]-9-yl)vinyl)pyridin-3-yl)benzonitrile 
• 1579952-87-6 (1R,3aR,4aR,4'R,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 
• 1579952-89-8 2-(6-((E)-2-((1R,3aR,4aR,4'R,8aR,9S,9aS)-1-methyl-2',3-dioxodecahydro-1H-spiro[naphtho[2,3-c]furan-6,4'-oxazolidin]-9-yl)vinyl)pyridin-3-yl)benzonitrile 

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.