89-25-8Relevant articles and documents
Structure and extractive ability of 1-alkyl- and 3-methyl-1-phenyl-2- pyrazolin-5-ones
Lesnov,Sazonova,Pavlov
, p. 298 - 302 (2005)
Extractive ability of 1-substituted 3-methylpyrazol-5-ones (LH) is studied. From acidic chloride complexes, ionic thallium(III) associates (LH 2)[TlCl4] are extracted; from trichloroacetate, coordination scandium complexes Sc(LH)4(CCl3COO) 3; and from ammine, copper(II) complexes CuL2. The extractive ability decreases in the order R = C7H15 > C6H13 > C5H11 > C 6H5 > C4H9. 2005 Pleiades Publishing, Inc.
Synthesis and crystal structure of 5-chloro-3-methyl-1-phenyl-1H-pyrazole- 4-carbaldehyde
Xu, Cun-Jin,Shi, Yan-Qin
, p. 1816 - 1819 (2011)
The title compound, 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehyde 2, was prepared in a series of syntheses to produce new pyrazole derivatives, and its crystal structure was determined by X-ray diffraction method. The crystal belongs to monoclinic
Synthesis and Herbicidal Activity of 5-Heterocycloxy-3-methyl-1-substituted-1H-pyrazoles
Kang, Jing,Yue, Xia Li,Chen, Chang Shui,Li, Jian Hong,Ma, Hong Ju
, (2016)
With the objective of finding valuable herbicidal candidates, a series of new 5-heterocycloxy- 3-methyl-1-substituted-1H-pyrazoles were synthesized and their herbicidal activities were evaluated. The bioassay results showed that some compounds exhibited e
Click inspired novel pyrazole-triazole-persulfonimide & pyrazole-triazole-aryl derivatives; Design, synthesis, DPP-4 inhibitor with potential anti-diabetic agents
Nidhar, Manisha,Khanam, Shaziya,Sonker, Priyanka,Gupta, Priya,Mahapatra, Archisman,Patil, Swaraj,Yadav, Brijesh Kumar,Singh, Rahul Kumar,Kumar Tewari, Ashish
supporting information, (2022/01/22)
This work presented the first report on designing, synthesizing of novel pyrazole-triazole-persulfonimide (7a-i) and pyrazole-triazole-aryl derivatives (8a-j) via click reaction using CuI catalyst and evaluated for their anti-diabetic activity and DPP-4 i
Discovery of novel inhibitors of human phosphoglycerate dehydrogenase by activity-directed combinatorial chemical synthesis strategy
Gou, Kun,Luo, Youfu,Luo, Yuan,Sun, Qingxiang,Tan, Yuping,Tao, Lei,Zhao, Yinglan,Zhou, Xia,Zhou, Yue,Zuo, Zeping
, (2021/07/26)
Serine, the source of the one-carbon units essential for de novo purine and deoxythymidine synthesis plays a crucial role in the growth of cancer cells. Phosphoglycerate dehydrogenase (PHGDH) which catalyzes the first, rate-limiting step in de novo serine biosynthesis has become a promising target for the cancer treatment. Here we identified H-G6 as a potential PHGDH inhibitor from the screening of an in-house small molecule library based on the enzymatic assay. We adopted activity-directed combinatorial chemical synthesis strategy to optimize this hit compound. Compound b36 was found to be the noncompetitive and the most promising one with IC50 values of 5.96 ± 0.61 μM against PHGDH. Compound b36 inhibited the proliferation of human breast cancer and ovarian cancer cells, reduced intracellular serine synthesis, damaged DNA synthesis, and induced cell cycle arrest. Collectively, our results suggest that b36 is a novel PHGDH inhibitor, which could be a promising modulator to reprogram the serine synthesis pathway and might be a potential anticancer lead worth further exploration.
Electrochemical synthesis of versatile ammonium oxides under metal catalyst-, exogenous-oxidant-, and exogenous-electrolyte-free conditions
Yuan, Yong,Li, Liang-Sen,Zhang, Lin,Wang, Feng,Jiang, Lin,Zuo, Lin,Wang, Qi,Hu, Jian-Guo,Lei, Aiwen
supporting information, p. 2768 - 2771 (2021/03/23)
An electrochemical oxidative cross-coupling reaction between 2.5-substituted-pyrazolin-5-ones and ammonium thiocyanate has been developed, which resulted in a series of unprecedented cross-coupling products under metal catalyst-, exogenous-oxidant-, and exogenous-electrolyte-free conditions. It is worth noting that since the resulting cross-coupling products are nearly insoluble in MeCN, the pure product could be afforded without silica gel column purification. In addition, the prepared ammonium oxides are versatile building blocks for synthesizing functionalized pyrazole derivatives.
Preparative, mechanistic and tautomeric investigation of 1-phenyl and 1-methyl derivative of 3-methyl-5-pyrazolone
Fakhraian, Hossein,Nafari, Yaser
, (2021/04/19)
1-Phenyl and 1-methyl derivative of 3-methyl-5-pyrazolone were prepared quantitatively via a scalable solvent-free reaction of corresponding hydrazine derivative with ethyl acetoacetate. Different mechanisms have been proposed for the reaction of hydrazine derivatives (methyl or phenyl) with ethyl acetoacetate and also the tautomeric aspects of the targeted compounds have been discussed. Graphical abstract: [Figure not available: see fulltext.] Synopsis: 13C NMR and quantitative proportional amount of different tautomeric forms of 1,3-dimethyl-5-pyrazolone in DMSO-d6.
Edaravone preparation method
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Paragraph 0014; 0026-0045, (2021/10/27)
To the preparation method of edaravone, hydrazine and ethyl acetoacetate are taken as raw materials to carry out cyclization reaction under a solvent-free condition, and water is reduced. The acetic acid, absolute ethyl alcohol and other solvents are intr
Edaravone preparation method
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Paragraph 0026-0042, (2021/11/26)
The edaravone preparation method comprises the following steps: S1) mixing phenylhydrazine and ethyl acetoacetate, and carrying out solvent-free reaction. S2) After the end of the reaction. A solvent is added to the reaction system for crystallization and
Design, synthesis, antibacterial evaluation and molecular docking studies of novel pyrazole/1,2,4-oxadiazole conjugate ester derivatives
Depa, Navaneetha,Erothu, Harikrishna
, p. 1087 - 1098 (2021/02/26)
The development of new antimicrobial drugs is most needed due to rapid growth in global antimicrobial resistance. Thus, in this context, a series of novel pyrazole/1,2,4-oxadiazole conjugate ester derivatives (7a–j) was synthesized. All the derivatives we
