64300-28-3Relevant academic research and scientific papers
Nitrosylsulfuric acid in the synthesis of 5-chloroisoxazoles from 1,1-dichlorocyclopropanes
Bondarenko, Oksana B.,Garaev, Zaur M.,Komarov, Arseniy I.,Kuznetsova, Lyubov I.,Gutorova, Svetlana V.,Skvortsov, Dmitry A.,Zyk, Nikolai V.
, p. 419 - 420 (2019/08/20)
Nitrosylsulfuric acid is shown to be a usable reagent for the synthesis of 5-chloroisoxazoles from readily available 1,1-di-chlorocyclopropanes via nitrosation–heterocyclization reaction. A cytotoxicity of some of the prepared 5-chloroisoxazoles towards M
Transformations of gem-dichloroarylcyclopropanes in the reaction with NOCl·2SO3. Synthesis of 3-aryl-5-chloroisoxazoles
Bondarenko,Gavrilova,Murodov,Zefirov,Zyk
, p. 186 - 194 (2013/07/25)
Nitrosation with complex NOCl·2SO3 of gem-dichloroarylcyclopropanes containing acceptor substituents in the aromatic ring proceeded chemo- and regioselectively affording 3-aryl-5-chloroisoxazoles in high yields. The presence of donor substituents complicated the reaction by the occurrence of competing processes.
Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1)
Nantermet, Philippe G,Barrow, James C.,Lundell, George F.,Pellicore, Janetta M.,Rittle, Kenneth E.,Young, MaryBeth,Freidinger, Roger M.,Connolly, Thomas M.,Condra, Cindra,Karczewski, Jerzy,Bednar, Rodney A.,Gaul, Stanley L.,Gould, Robert J.,Prendergast, Kris,Selnick, Harold G.
, p. 319 - 323 (2007/10/03)
The synthesis and biological evaluation of a series of nonpeptidic small molecule antagonists of the human platelet thrombin receptor (PAR-1) are described. Optimization of the 5-amino-3-arylisoxazole lead resulted in an approximate 100-fold increase in potency. The most potent of these compounds (54) inhibits platelet activation with IC50s of 90 nM against the thrombin receptor agonist peptide (TRAP) and 510 nM against thrombin as the agonist. Further, antagonist 54 fully blocks platelet aggregation stimulated by 1 nM thrombin for 10 min.
