41927-54-2Relevant academic research and scientific papers
Base promoted direct C4-arylation of 4-substituted-pyrazolin-5-ones with diaryliodonium salts
Mao, Song,Geng, Xu,Yang, Yang,Qian, Xiaofei,Wu, Shengying,Han, Jianwei,Wang, Limin
, p. 36390 - 36393 (2015/05/05)
A metal-free approach for the C4-arylation of 4-substituted-pyrazolin-5-ones with diaryliodonium salts was developed. The reaction proceeded smoothly at room temperature in the presence of DMAP (4-dimethylaminopyridine). As a result, a wide range of desir
New series of antiprion compounds: Pyrazolone derivatives have the potent activity of inhibiting protease-resistant prion protein accumulation
Kimata, Ayako,Nakagawa, Hidehiko,Ohyama, Ryo,Fukuuchi, Tomoko,Ohta, Shigeru,Suzuki, Takayoshi,Miyata, Naoki
, p. 5053 - 5056 (2008/03/13)
To find effective antiprion compounds, we synthesized and evaluated various pyrazolone derivatives. Seven of 19 compounds showed inhibition of PrP-res accumulation and the remarkably active compound 13 showed an IC50 value of 3 nM in both ScN2a and F3 cell lines. Findings from studies on physicochemical and biochemical properties suggest that the action mechanism of these compounds does not correlate with any antioxidant activities, any of hydroxyl radical scavenging activities, or any SOD-like activities.
Hydroxyl radical scavenging by edaravone derivatives: Efficient scavenging by 3-methyl-1-(pyridin-2-yl)-5-pyrazolone with an intramolecular base
Nakagawa, Hidehiko,Ohyama, Ryo,Kimata, Ayako,Suzuki, Takayoshi,Miyata, Naoki
, p. 5939 - 5942 (2007/10/03)
We synthesized various 3-methyl-1-phenyl-5-pyrazolone (edaravone) derivatives and evaluated their oxidation potential and hydroxyl radical scavenging activity. It was found 3-methyl-1-(pyridin-2-yl)-5-pyrazolone had a much higher ability to scavenge the radical than did edaravone itself. Its efficient radical scavenging activity was assumed to be due to the increase of its anion form, an active form, by a hydrogen-bonded intramolecular base.
One-pot synthesis of 5-(substituted-amino)pyrazoles
Dodd, Dharmpal S.,Martinez, Rogelio L.
, p. 4265 - 4267 (2007/10/03)
An efficient and mild one-pot synthesis of substituted 5-alkylamino and/or 5-(arylamino)pyrazoles is described. A suitably decorated β-ketoamide, an aryl or alkyl hydrazine and Lawesson's reagent are suspended in THF/Py and gently heated to yield the requisite 5-aminopyrazoles.
A novel route to 2,3-pyrazol-1(5H)-ones via palladium-catalyzed carbonylation of 1,2-diaza-1,3-butadienes
Boeckman Jr., Robert K.,Reed, Jessica E.,Ge, Ping
, p. 3651 - 3653 (2007/10/03)
Figure presented A novel Pd(0)-catalyzed carbonylation of both isolable 1,2-diaza-1,3-butadienes and those generated in situ by extrusion of SO2 and CO2 from heterocyclic precursors is described. The reaction proceeds at room temperature to 110°C under 1-2 atm of CO to afford 2,3-pyrazol-1(5H)-ones in good to excellent yields. The effect of catalyst structure and stability on the carbonylation reaction is evaluated.
