87813-03-4Relevant articles and documents
Reagents for Storage and Regeneration of Nonstabilized Azomethine Ylides: Spiroanthraceneoxazolidines
Buev, Evgeny M.,Moshkin, Vladimir S.,Sosnovskikh, Vyacheslav Y.
, p. 1764 - 1767 (2016/05/19)
Nonstabilized azomethine ylides are easily trapped by anthraquinone to form stable spiro-oxazolidines, which have an unusual ability to undergo a cycloreversion in the presence of other dipolarophiles at 120-150°C. All tested recycloadditions with carbonyl compounds and electron-poor alkenes occurred in moderate to high yields (41-92%). Moreover, increasing the reaction temperature to 210°C made it possible to obtain adducts with low reactive dipolarophiles.
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists
Young, Jonathan R.,Eid, Ronsar,Turner, Cherilyn,DeVita, Robert J.,Kurtz, Marc M.,Tsao, Kwei-Lan C.,Chicchi, Gary G.,Wheeldon, Alan,Carlson, Emma,Mills, Sander G.
, p. 5310 - 5315 (2008/03/11)
The preparation and structure-activity-relationships of novel pyrrolidine-carboxamides and oxadiazoles are described. Compounds in this series were found to be potent hNK1 antagonists in vitro and efficacious in vivo with minimal interactions with P450 liver enzymes. Oxadiazole analog 22 was determined to have excellent hNK1 binding affinity, functional activity, and a good PD response in vivo.
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: Discovery of the pyrrolidine scaffold and determination of its stereochemical requirements
Hale, Jeffrey J.,Budhu, Richard J.,Mills, Sander G.,MacCoss, Malcolm,Malkowitz, Lorraine,Siciliano, Salvatore,Gould, Sandra L.,DeMartino, Julie A.,Springer, Martin S.
, p. 1437 - 1440 (2007/10/03)
A series of 1,3,4-trisubstituted pyrrolidines was discovered to have the ability to displace [125I]-MIP-1α from the CCR5 receptor expressed on Chinese hamster ovary (CHO) cell membranes. CCR5 activity was found to be dependent on the regiochemi
