40040-65-1Relevant academic research and scientific papers
Diastereospecific Enantiodivergent Allylation of Pyrazolones as an Entry to β-Aminoamides
Demircan, Aysegül,Heberle, Martin,Peters, René,Pfeffer, Camilla,Wannenmacher, Nick,Wanner, Daniel M.,Yu, Xin
supporting information, (2022/04/25)
A diastereospecific enantiodivergent allylation of pyrazolones is reported which is catalyzed by a planar chiral pentaphenylferrocene based palladacycle. With the same catalyst batch both product enantiomers were selectively available. The method is applicable to structurally diverse substrates and gave products with enantiomeric excesses between 85 and 94%. In addition, we could show that pyrazolones are transformable into β-aminoamides.
Design, Synthesis, and Structure-Activity Relationship Study of Pyrazolones as Potent Inhibitors of Pancreatic Lipase
Zhang, Jing,Yang, Yang,Qian, Xing-Kai,Song, Pei-Fang,Zhao, Yi-Shu,Guan, Xiao-Qing,Zou, Li-Wei,Bao, Xiaoze,Wang, Hong
supporting information, p. 1600 - 1604 (2021/03/03)
Pancreatic lipase (PL), a key target for the prevention and treatment of obesity, plays crucial roles in the hydrolysis and absorption of in dietary fat. In this study, a series of pyrazolones was synthesized, and their inhibitory effects against PL were
Discovery of pyrazolones as novel carboxylesterase 2 inhibitors that potently inhibit the adipogenesis in cells
Qian, Xing-Kai,Zhang, Jing,Song, Pei-Fang,Zhao, Yi-Su,Ma, Hong-Ying,Jin, Qiang,Wang, Dan-Dan,Guan, Xiao-Qing,Li, Shi-Yang,Bao, XiaoZe,Zou, Li-Wei
, (2021/05/10)
Carboxylesterase 2 (CES2) is one of the most important Phase I drug metabolizing enzymes in the carboxylesterase family. It plays crucial roles in the bioavailability of oral ester prodrugs and the therapeutic effect of some anticancer drugs such as irino
Organocatalytic Amination of Pyrazolones with Azodicarboxylates: Scope and Limitations
Formánek, Bed?ich,?eferna, Vít,Meazza, Marta,Rios, Ramon,Patil, Mahendra,Vesely, Jan
supporting information, p. 2362 - 2366 (2021/03/16)
The organocatalytic amination of pyrazol-5-ones with azodicarboxylates (catalyzed by quinine) is reported. This asymmetric process furnishes enantiomerically enriched hydrazine adducts containing quaternary stereocenters in high yields (74–96 %) and enant
Tunable Aerobic Oxidative Hydroxylation/Dehydrogenative Homocoupling of Pyrazol-5-ones under Transition-Metal-Free Conditions
Sheng, Xuguang,Zhang, Jinlong,Yang, Huameng,Jiang, Gaoxi
, p. 2618 - 2621 (2017/05/24)
A practical and tunable transition-metal-free aerobic oxidation of pyrazol-5-ones preparing either 4-hydroxypyrazoles (via C-H hydroxylation) or bispyrazoles (via dehydrogenative homocoupling) is described. The K2CO3/dioxane reagent system predominately promoted hydroxylation to deliver the α-hydroxylated pyrazoles. In contrast, the formation of bispyrazoles was overwhelmingly preferred with CH3CN as the reaction medium without any additives.
Alkynylation of heterocyclic compounds using hypervalent iodine reagent
Kamlar,Císa?ová,Vesely
, p. 2884 - 2889 (2015/04/27)
The alkynylation of various nitrogen- and/or sulphur-containing heterocyclic compounds using hypervalent iodine TMS-EBX by utilization of tertiary amines under mild conditions is described. The developed metal-free methodology furnishes the corresponding alkynylated heterocycles bearing quaternary carbon in high yields.
FACILE SYNTHESIS OF 4-SUBSTITUTED 2-PYRAZOLIN-5-ONES UNDER PHASE TRANSFER CATALYSIS
Shiba, Sayed A.,Harb, Nagwa M.S.,El-Kassaby, Mohamad A.,Hassan, Mohamed A.,Abou El-Regal, Mohsen M.K.
, p. 15 - 20 (2007/10/03)
Nucleophilic displacement of organohalogen compounds by 2-pyrazolin-5-ones (1) in absence/or presence of carbon disulphide or phenyl isothiocyanate under phase transfer catalysis conditions have been studied to give 4-substituted-2-pyrazolin-5-ones (2-8)
TAUTOMERISM OF 1-PHENYL-3-METHYL-4-BENZYL-5-PYRAZOLONE
Vinokurov, V. G.,Zykov, D. A.,Kirsanova, Z. D.,Rozenberg, S. G.,Troitskaya, V. S.,et al.
, p. 288 - 291 (2007/10/02)
The tautomerism of 1-phenyl-3-methyl-4-benzyl-5-pyrazolone - a side product in the reaction of acetoacetic ester with benzaldehyde phenylhydrazone - was studied by IR and PMR spectroscopy, and its thermodynamic characteristics were determined.
