849674-12-0Relevant articles and documents
Asymmetric Synthesis of Merck's Potent hNK1Antagonist and Its Stereoisomers via Tandem Acylation/[3,3]-Rearrangement of 1,2-Oxazine N-Oxides
Dorokhov, Valentin S.,Nelyubina, Yulia V.,Ioffe, Sema L.,Sukhorukov, Alexey Yu.
, p. 11060 - 11071 (2020/10/12)
An asymmetric total synthesis of Merck's hNK1 antagonist and three of its stereoisomers was accomplished in 10 steps. The synthesis involves a stereoselective assembly of 1,2-oxazine N-oxide by the [4 + 2]-cycloaddition, site-selective C-H oxygenation usi
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists
Jiang, Jinlong,Bunda, Jaime L.,Doss, Geoge A.,Chicchi, Gary G.,Kurtz, Marc M.,Tsao, Kwei-Lan C.,Tong, Xinchun,Zheng, Song,Upthagrove, Alana,Samuel, Koppara,Tschirret-Guth, Richard,Kumar, Sanjeev,Wheeldon, Alan,Carlson, Emma J.,Hargreaves, Richard,Burns, Donald,Hamill, Terence,Ryan, Christine,Krause, Stephen M.,Eng, WaiSi,DeVita, Robert J.,Mills, Sander G.
experimental part, p. 3039 - 3046 (2010/03/03)
3-[(3aR,4R,5S,7aS)-5-{(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy} -4-(4-fluorophenyl)octahydro-2H-isoindol-2-yl]-cyclopent-2-en-1-one (17) is a high affinity, brain-penetrant, hydroisoindoline-based neurokinin-1 (NK1) receptor antagonist with a long ce
Process for making hydroisoindoline tachykinin receptor antagonists
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Page/Page column 13; 14, (2008/06/13)
The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.