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96-96-8Relevant academic research and scientific papers
Fused tricyclic derivative as FGFR4 inhibitor
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, (2021/05/12)
The present invention provides a fused tricyclic derivative that is the selective inhibitor of fibroblast growth factor receptor 4 (FGFR4), a pharmaceutical composition containing the compound, a method of making the compound and a method of treating cell proliferative diseases, such as cancer, using the compounds of the invention.
Method for synthesizing 4-methoxy-2-nitroaniline by adopting continuous flow reactor
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, (2020/10/05)
The invention relates to the technical field of organic synthesis, and discloses a method for synthesizing 4-methoxy-2-nitroaniline by using a continuous flow reactor. The method comprises the following steps: S1, respectively adding a 4-methoxyaniline solution and acetic anhydride into a continuous flow reactor I, and carrying out an acetylation reaction to obtain a reaction solution I containing4-methoxyacetanilide; S2, respectively adding a nitration reagent and the reaction solution I into a continuous flow reactor II, and carrying out a nitration reaction to obtain a reaction solution IIcontaining 4-methoxy-2-nitroacetanilide; S3, respectively adding hydrolysate and the reaction solution II into a continuous flow reactor III, and carrying out a hydrolysis reaction to obtain a reaction solution III containing 4-methoxy-2-nitroaniline; and S4, carrying out post-treatment on the reaction solution III to obtain 4-methoxy-2-nitroaniline. The method is high in reaction speed, small inamount of byproduct 4-methoxy-3-nitroaniline, high in heat and mass transfer efficiency, high in reaction safety, high in selectivity, high in yield and purity and convenient in after-treatment.
Sodium persulfate-promoted site-selective synthesis of mononitroarylamines under transition-metal-free conditions
Xie, De-Xun,Yu, Hui-Juan,Liu, Hui,Xue, Wei-Cai,Qin, Yuan-Shou,Shao, Guang
, p. 1157 - 1165 (2019/01/24)
A practical preparation of nitroarylamines from protected arylamines was herein disclosed. In this system, sodium nitrite acted as a nitration reagent in the presence of sodium persulfate without any transition-metal catalysts. This efficient site-selective protocol took place at room temperature for a short time through a free radical pathway.
A O-nitro to the preparation method of the anisidine
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, (2018/07/15)
The invention relates to a O-nitro to anisidine preparation method. Characterized in that to the anisidine as raw materials, by acetylation, mixed acid nitration to obtain the 4 - methoxy - 2 - nitro acetanilide, and hydrolyzed to from 2 - nitro - 4 - methoxybenzene elimination and to acetaminophen as raw materials, by methylation, antirust, the reduction reaction of the nitro to synthetic O-anisidine.
NOVEL FYN KINASE INHIBITORS
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, (2017/03/28)
The present invention relates to the novel therapies to treat neurodegenerative diseases such as Parkinson's disease (PD). The present invention relates to novel small molecule inhibitors of Fyn Kinase and for testing activity against Parkinsons's disease models compounds that inhibit Fyn kinase having the following formula. (I)
Salicylic Acid-Catalyzed One-Pot Hydrodeamination of Aromatic Amines by tert-Butyl Nitrite in Tetrahydrofuran
Felipe-Blanco, Diego,Alonso, Francisco,Gonzalez-Gomez, Jose C.
, p. 2857 - 2863 (2017/08/23)
A significant acceleration in the hydrodeamination of in situ formed diazonium salts (from aromatic amines) has been observed in the presence of 10-mol% salicylic acid, using tetrahydrofuran as the hydrogen donor. The reaction proceeds efficiently at 20 °C for a wide range of substituted anilines, even at 10-mmol scale, without any other additive. The same protocol has been adapted to the selective deuterodeamination of some aromatic amines. Control experiments clearly show that aryl radicals are involved in the reaction mechanism. (Figure presented.).
Palladium(II)-catalyzed, heteroatom-directed, regioselective C-H nitration of anilines using pyrimidine as a removable directing group
Pawar, Govind Goroba,Brahmanandan, Abhilashamole,Kapur, Manmohan
, p. 448 - 451 (2016/02/18)
A new palladium-catalyzed, heteroatom-directed strategy for C-H nitration of anilines is described. This C-H functionalization reaction is highly ortho-selective and results in very good yields. The highlight of the work is the use of pyrimidine as the removable directing group. This approach constitutes one of the rare methods of ortho-nitration of anilines, a reaction that is normally very difficult to achieve via traditional approaches.
Indole and indazole compounds as an inhibitor of cellular necrosis
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Paragraph 0339; 0344-0346; 0349, (2016/10/08)
The present invention refers to a formula (1) compounds of, pharmaceutically acceptable salts or isomers thereof thereof, and characterized by by containing as active ingredients-associated diseases, cell death and method for the prevention or treatment of relates and compositions. [Formula 1] In formula said R 1, R 2, R 3, R 4, R 5, R 6, A, X, n and m to equal the specification.
Cyclometalated iridium(III) bipyridyl-phenylenediamine complexes with multicolor phosphorescence: Synthesis, electrochemistry, photophysics, and intracellular nitric oxide sensing
Law, Wendell Ho-Tin,Leung, Kam-Keung,Lee, Lawrence Cho-Cheung,Poon, Che-Shan,Liu, Hua-Wei,Lo, Kenneth Kam-Wing
, p. 1316 - 1329 (2014/06/09)
We present a new class of phosphorescent cyclometalated iridium(III) bipyridyl-phenylenediamine complexes [Ir(N^C)2(bpy-DA)](PF 6) (bpy-DA=4-(N-(2-amino-5-methoxyphenyl)aminomethyl)-4′- methyl-2,2′-bipyridine; HN^C=2-(2,4-difluorophenyl)pyridine (Hdfppy) (1-a), 2-phenylpyridine (Hppy) (2-a), 2-phenylquinoline (Hpq) (3-a), 2-phenylcinchoninic acid methyl ester (Hpqe) (4-a)) and their triazole counterparts [Ir(N^C)2(bpy-T)](PF6) (bpy-T=4-((6- methoxybenzotriazol-1-yl)methyl)-4′-methyl-2,2′-bipyridine; HN^C=Hdfppy (1-b), Hppy (2-b), Hpq (3-b), Hpqe (4-b)). Upon photoexcitation, the diamine complexes exhibited fairly weak green to red phosphorescence under ambient conditions whereas the triazole derivatives emitted strongly. The photophysical properties of complexes 2-a and 2-b have been studied in more detail. Upon protonation, the diamine complex 2-a displayed increased emission intensity, but the emission properties of its triazole counterpart complex 2-b were independent on the pH value of the solution. Also, complex 2-a was found to be readily converted into complex 2-b upon reaction with NO under aerated conditions, resulting in substantial emission enhancement of the solution. The reaction was highly specific toward NO over other reactive oxygen and nitrogen species (RONS) as revealed by spectroscopic analyses. The lipophilicity and cellular uptake efficiency of the diamine complexes have been examined and correlated to their molecular structures. Also, cell-based assays showed that these complexes were noncytotoxic toward human cervix epithelioid carcinoma (HeLa) cells (at 10 μM, 4 h, percentage survival ≈80-95-%). Additionally, the diamine complexes have been used to visualize intracellular NO generated both exogenously in HeLa cells and endogenously in RAW 264.7 murine macrophages by laser-scanning confocal microscopy. Visualizing NO: Phosphorescent cyclometalated iridium(III) bipyridyl-phenylenediamine complexes have been designed as intracellular NO sensors. They react selectively with NO over other reactive oxygen and nitrogen species and are converted into their triazole counterparts, resulting in significant emission enhancement. The diamine complexes show low cytotoxic activity and are capable of sensing intracellular NO generated exogenously in HeLa cells and endogenously in RAW 264.7 murine macrophages.
Rhenium(I) polypyridine diamine complexes as intracellular phosphorogenic sensors: Synthesis, characterization, emissive behavior, biological properties, and nitric oxide sensing
Choi, Alex Wing-Tat,Yim, Vicki Man-Wai,Liu, Hua-Wei,Lo, Kenneth Kam-Wing
supporting information, p. 9633 - 9642 (2014/08/18)
We report the development of a series of rhenium(I) polypyridine complexes appended with an electron-rich diaminoaromatic moiety as phosphorogenic sensors for nitric oxide (NO). The diamine complexes [Re(N^N)(CO)3(py-DA)] [PF6] (py-DA=3-(N-(2-amino-5-methoxyphenyl)aminomethyl)pyridine; N^N=1,10-phenanthroline (phen) (1a), 3,4,7,8-tetramethyl-1,10-phenanthroline (Me4-phen) (2a), 4,7-diphenyl-1,10-phenanthroline (Ph 2-phen) (3a)) have been synthesized and characterized. In contrast to common rhenium(I) diimines, these diamine complexes were very weakly emissive due to quenching of the triplet metal-to-ligand charge-transfer ( 3MLCT) emission by the diaminoaromatic moiety through photoinduced electron transfer (PET). Upon treatment with NO, the complexes were converted into the triazole derivatives [Re(N^N)(CO)3(py-triazole)][PF 6] (py-triazole=3-((6-methoxybenzotriazol-1-yl)methyl)pyridine; N^N=phen (1b), Me4-phen (2b), Ph2-phen (3b)), resulting in significant emission enhancement (I/I0≈60). The diamine complexes exhibited high reaction selectivity to NO, and their emission intensity was found to be independent on pH. Also, these complexes were effectively internalized by HeLa cells and RAW264.7 macrophages with negligible cytotoxicity. Additionally, the use of complex 3a as an intracellular phosphorogenic sensor for NO has been demonstrated. Emission turned ON for NO: A series of rhenium(I) polypyridine complexes functionalized with an electron-rich diaminoaromatic moiety has been developed as a new class of phosphorogenic sensors for NO. Upon treatment with NO, the weakly emissive complexes were converted into the strongly emissive triazole derivatives, resulting in significant emission enhancement (I/I0≈60; see figure). Experiments showed that the diamine complexes can sense NO that is 1) generated exogenously by NOC-7 in HeLa cells and 2) produced endogenously in RAW264.7 macrophages.