76155-27-6Relevant articles and documents
Novel nitrile oxide cycloaddition approach towards papuamine: Stereoselective synthesis of a potentially useful trans-hydrindane intermediate
Saha, Arabinda,Bhattacharjya, Anup
, p. 495 - 496 (1997)
In a potentially useful approach to the marine alkaloid papuamine 1, a known trans-hydrindane intermediate 17 has been synthesised in racemic form using a model sequence of reactions involving a nitrile oxide cycloaddition as a key step.
Carbonylation of ethylenically unsaturated compounds
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Page/Page column 37, (2016/06/01)
A process for the carbonylation of ethylenically unsaturated compounds including vinyl esters and a process for the production of 3-hydroxy propanoate esters or acids. The process comprises reacting said compound with carbon monoxide in the presence of a source of hydroxyl groups and of a catalyst system. The catalyst system is obtainable by combining: (a) a metal of Group 8, 9 or 10 or a compound thereof: and (b) a bidentate ligand of general formula (I): X1(X2)-Q2-A-R—B-Q1-X3(X4).
Discovery of octahydroindenes as PAR1 antagonists
Lee, Sunkyung,Song, Jong-Hwan,Park, Chul Min,Kim, Jin-Seok,Jeong, Ji-Hye,Cho, Woo-Young,Lim, Dong-Chul
supporting information, p. 1054 - 1058 (2013/12/04)
Octahydroindene was identified as a novel scaffold for protease activated receptor 1 (PAR1) antagonists. Herein, the 2-position (C2) was explored for structure-activity relationship (SAR) studies. Compounds 14, 19, and 23b showed IC50 values of 1.3, 8.6, and 2.7 nM in a PAR1 radioligand binding assay, respectively, and their inhibitory activities on platelet activation were comparable to that of vorapaxar in a platelet rich plasma (PRP) aggregation assay. This series of compounds showed high potency and no significant cytotoxicity; however, the compounds were metabolically unstable in both human and rat liver microsomes. Current research efforts are focused on optimizing the compounds to improve metabolic stability and physicochemical properties as well as potency.