92-43-3Relevant academic research and scientific papers
Biguanide derivatives, pharmaceutical composition, preparation method and application
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Paragraph 0035-0037, (2019/01/14)
The invention belongs to the field of medicine and particularly relates to biguanide derivatives, pharmaceutical composition, a preparation method and an application. The biguanide derivatives are compounds with the structure shown in the description, or pharmaceutically acceptable salts, solvates, isomers, esters and predrugs of the compounds. The compounds can remarkably inhibit proliferation and migration of tumor cells, IC50 is greatly lower than that of metformin and phenformin before derivatization, the compound 11 has the highest activity, and activity of the compounds in UMUC3, T24 andA2780 cells is more than 300-800 times that of metformin, and the compounds have good application prospect in antitumor drugs.
A convenient one-pot synthesis of 1-aryl-substituted 4-iodopyrazol-3-ols via aromatisation and oxidative iodination reactions
Liu, Jingjing,Yang, Shanguang,Dong, Ruimei,Jin, Zhudan,Wang, Mingliang
, p. 24 - 27 (2018/02/28)
A convenient and economical one-pot synthesis of a series of new 1-aryl-substituted 4-iodopyrazole-3-ols from easily available pyrazolidin- 3-ones in the presence of sodium iodide, 30% solution of hydrogen peroxide and a catalytic amount of sulfuric acid in dichloromethane via aromatisation and oxidative iodination reactions are described. This protocol has the advantages of high atom economy, costeffectiveness, short reaction time and environmental friendliness.
Amide compound and application thereof
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Paragraph 0144-0148, (2018/09/28)
The invention provides an amide compound and application thereof. Compared with compounds in the prior art, the compound disclosed by the invention has the advantage that the bactericidal activity isobviously improved. The invention is expected to develop a bactericide which is in novel structure and is used for controlling diseases in agriculture, forestry or sanitation.
Synthesis, fungicidal activity, structure-activity relationship and density functional theory studies of novel oxime ether derivatives containing 1-aryl-3-oxypyrazoles
Lv, Kunzhi,Liu, Yuanyuan,Li, Yi,Xu, Guanghui,Pan, Xuechun,Li, Fangshi,Chen, Kai,Huang, Bin,Yang, Yaping
, p. 594 - 600 (2015/11/27)
A series of 16 oxime ether derivatives containing 1-aryl-3-oxypyrazoles were synthesised, and the structure of one of them, (E)-methyl 2-(2-({(1-(4-chlorophenyl)-1H-pyrazol-3-yl)-oxy}methyl)phenyl)-2-(methoxyimino)acetate was determined by X-ray diffraction crystallography. Preliminary bioassays indicated that some of these compounds exhibited very good fungicidal activities against Rhizoctonia solani, especially the ester 2-(2-({(1-(4-chlorophenyl)-1H-pyrazol-3-yl)-oxy}methyl)phenyl)-2-(methoxyimino)acetate, which displayed greater activity than control compound pyraclostrobin at a dosage of 0.1 μg mL-1. The relationship between structure and fungicidal activity was discussed. Density functional theory studies of the 3-methyl heterocyclic ester and the 4-chorophenyl heterocyclic N-methylamide were carried out and the results discussed in terms of the wide difference in fungicidal activity shown by each compound.
DMF-catalyzed direct and regioselective C-H functionalization: Electrophilic/nucleophilic 4-halogenation of 3-oxypyrazoles
Liu, Yuanyuan,He, Guangke,Chen, Kai,Jin, Yin,Li, Yufeng,Zhu, Hongjun
supporting information; experimental part, p. 5323 - 5330 (2011/11/13)
A novel, straightforward, and highly regioselective 4-chlorination of 3-oxypyrazole derivatives in boiling thionyl chloride (SOCl2) in the presence of catalytic N,N-dimethylformamide (DMF) has been developed. This reaction likely proceeds through a DMF-catalyzed electrophilic/nucleophilic chlorination mechanism and involves electrophilic attack by SOCl2 and nucleophilic substitution by Cl- as the key steps. Based on this mechanism, the corresponding 4-bromination and 4-iodination of 3-oxypyrazoles have also been achieved in good yield by adding Br- and I -, respectively, to the reaction system. This halogenation method enables quick access to many original 4-halo-3-oxypyrazole series. A novel DMF-catalyzed electrophilic/nucleophilic 4-halogenation of 3-oxypyrazole derivatives has been developed. This halogenation procedure provides quick access to many novel 4-halo-3-oxypyrazole series.
Synthesis, crystal structure and fungicidal activities of new type oxazolidinone-based strobilurin analogues
Li, Yuhao,Liu, Rui,Yan, Zhangwei,Zhang, Xiangning,Zhu, Hongjun
experimental part, p. 3341 - 3347 (2012/05/05)
A series of oxazolidinone-based strobilurin analogues were efficiently synthesized by the reaction of 3-(2-bromomethylphenyl) oxazolidin-2-one with 1-substituted phenyl-2H-pyrazolin-3-one. Their structures were confirmed and characterized by 1H-NMR, 13C-NMR, elemental analysis, and mass spectroscopy. In addition, the crystal structure of the target compound 3-(2-((1-phenyl-2H-pyrazol-3-yloxy)methyl)phenyl) oxazolidin-2-one was determined by single crystal X-ray diffraction. The bioassay results of these compounds indicated that some of the oxazolidin-2-one derivatives containing N-substituted phenyl 2H-pyrazol ring exhibited potential in vivo fungicidal activities against M. grisea at the dosage of 1 g L-1.
2-(4-pyrazolyloxy-pyrimidin-5-yl) acetic acid derivatives
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, (2008/06/13)
This invention relates to novel 2-(4-pyrazolyloxy-pyrimidin-5-yl) acetic acid derivatives of formula I STR1 wherein R1 is hydrogen, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C3-6 cycloalkyl, or di-C1-4 alkylamino, R2 is hydrogen, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, or di-C1-4 alkyl-amino, R3 is hydrogen or methyl, R4 is aryl, aryl-C1-4 alkyl, heteroaryl, or heteroaryl-C1-4 alkyl, wherein each of the aromatic rings may be optionally substituted; and X is CH or nitrogen; the use of such compounds for the control of phytopathogens, compositions for facilitating such use, and the preparation of the compounds of formula I.
