14346-13-5Relevant articles and documents
Discovery of HN37 as a Potent and Chemically Stable Antiepileptic Drug Candidate
Zhang, Yang-Ming,Xu, Hai-Yan,Hu, Hai-Ning,Tian, Fu-Yun,Chen, Fei,Liu, Hua-Nan,Zhan, Li,Pi, Xiao-Ping,Liu, Jie,Gao, Zhao-Bing,Nan, Fa-Jun
, p. 5816 - 5837 (2021)
We previously reported that P-retigabine (P-RTG), a retigabine (RTG) analogue bearing a propargyl group at the nitrogen atom in the linker of RTG, displayed moderate anticonvulsant efficacy. Recently, our further efforts led to the discovery of HN37 (pynegabine), which demonstrated satisfactory chemical stability upon deleting the ortho liable -NH2 group and installing two adjacent methyl groups to the carbamate motif. HN37 exhibited enhanced activation potency toward neuronal Kv7 channels and high in vivo efficacy in a range of pre-clinical seizure models, including the maximal electroshock test and a 6 Hz model of pharmacoresistant limbic seizures. With its improved chemical stability, strong efficacy, and better safety margin, HN37 has progressed to clinical trial in China for epilepsy treatment.
A capping agent dissolution method for the synthesis of metal nanosponges and their catalytic activity towards nitroarene reduction under mild conditions
Ghosh, Sourav,Jagirdar, Balaji R.
, p. 17401 - 17411 (2018)
We report a general strategy for the synthesis of metal nanosponges (M = Ag, Au, Pt, Pd, and Cu) using a capping agent dissolution method where addition of water to the M@BNHx nanocomposite affords the metal nanosponges. The B-H bond of the BNHx polymer gets hydrolysed upon addition of water and produces hydrogen gas bubbles which act as dynamic templates leading to the formation of nanosponges. The rate of B-H bond hydrolysis has a direct impact on the final nanostructure of the materials. The metal nanosponges were characterized using powder XRD, electron microscopy, XPS, and BET surface area analyzer techniques. The porous structure of these nanosponges offers a large number of accessible surface sites for catalytic reactions. The catalytic activity of these metal nanosponges has been demonstrated for the reduction of 4-nitrophenol where palladium exhibits the highest catalytic activity (k = 0.314 min?1). The catalytic activity of palladium nanosponge was verified for the tandem dehydrogenation of ammonia borane and the hydrogenation of nitroarenes to arylamines in methanol at room temperature. The reduction of various substituted nitroarenes was proven to be functional group tolerant except for a few halogenated nitroarenes (X = Br and I) and >99% conversion was noted within 30-60 min with high turnover frequencies (TOF) at low catalyst loading (0.1 mol%). The catalyst could be easily separated out from the reaction mixture via centrifugation and was recyclable over several cycles, retaining its porous structure.
Palladium nanoparticles stabilized by aqueous vesicles self-assembled from a PEGylated surfactant ionic liquid for the chemoselective reduction of nitroarenes
Xu, Zhu-bing,Lu, Guo-ping,Cai, Chun
, p. 57 - 60 (2017/06/06)
Vesicles self-assembled from an aqueous PEGylated surfactant ionic liquid solution can be applied for stabilizing palladium nanoparticles, which prove to be an efficient catalytic system for chemoselective hydrogen transfer of nitroarenes using hydrazine hydrate as a hydrogen source. The particle sizes of vesicles are decreased with the increase of ionic liquid's concentrations and relatively small particle sizes are beneficial to the reduction. Moreover, the aqueous catalytic system still stays in reactor by simple extraction, and is reused without further treatment.
Magnetically Recoverable Gold Nanorods as a Novel Catalyst for the Facile Reduction of Nitroarenes Under Aqueous Conditions
Lamei, Kamran,Eshghi, Hossein,Bakavoli, Mehdi,Rostamnia, Sadegh
, p. 491 - 501 (2017/02/18)
Abstract: In this work, cysteine-functionalized Fe3O4@Carbon magnetic nanoparticles were used for the synthesis of gold nanorods. Fe3O4@C nanoparticles were first prepared by synthesis of Fe3O4magnetic nanoparticles (MNPs), and then carbon-coated MNPs (Fe3O4@C) were synthesized by glucose carbonization using a hydrothermal method. Finally, the gold NRs were loaded on the modified surface of Fe3O4@C MNPs. The designed magnetically recoverable gold nanorods, after full characterization by FTIR, SEM, TEM, TGA, VSM, XRD, and ICP-OES, were applied to the reduction of nitroarenes. The Fe3O4@C@Cys–Au nanorods showed higher performance than Fe3O4@C@Cys–Au nanospheres in a selective facile reduction of nitroarenes to the corresponding aminoarenes in aqueous medium at room temperature using NaBH4. Graphical Abstract: [Figure not available: see fulltext.]
Phenylenediamine derivatives and Method for manufacturing thereof
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Paragraph 0087-0096, (2017/06/02)
The present invention relates to a phenyleneamine-based compound and a producing method thereof and, more specifically, to a phenyleneamine-based compound which can replace existing para-phenylenediamine, has high purity by reducing the generation amount of waste water and using a hydrocarbon solvent, and has low initial investment costs and can reduce the production cost because the collection of the hydrocarbon solvent is easy, and to a producing method thereof.COPYRIGHT KIPO 2017
A liquid phase catalytic hydrogenation preparation of 2,5-di- amino-benzene nitrile method
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Paragraph 0034-0039, (2017/01/31)
The invention discloses a method for preparing 2, 5-diamino cyanophenyl through liquid phase catalytic hydrogenation. The method comprises steps of firstly, adding 2-cyanogroup-4 nitroaniline, a reaction solvent, a catalyst and a cocatalyst into a high pressure reaction kettle, reacting till no hydrogen is absorbed, and then filtering the reacted reaction material, so as to obtain a filtrate; secondly, settling and crystallizing the filtrate so as to obtain solid-liquid mixture; thirdly, under the protection of nitrogen, separating solid from liquid in the solid-liquid mixture, putting the solid in a vacuum drying box for drying, then distilling at reduced pressure, so as to obtain 2, 5-diamino cyanophenyl; fourthly, concentrating the separated liquid, then processing the concentrated filtrate according to the second and third steps. The method adopts raney nickel or loaded noble metal catalyst for liquid phase catalytic hydrogenation, also adopts the cocatalyst, and successfully prepares the high quality and high yield 2, 5-diamino cyanophenyl by hydrogenation, recrystalization, concentration and distillation at reduced pressure; the purity of the prepared 2, 5-diamino cyanophenyl is not less than 99.5%, and the yield of the prepared 2, 5-diamino cyanophenyl is not less than 90%.
Chemoselective transfer hydrogenation of nitroarenes by highly dispersed Ni-Co BMNPs
Zhang, Jia-Wei,Lu, Guo-Ping,Cai, Chun
, p. 25 - 29 (2016/06/13)
Highly dispread Ni-Co bimetallic nanoparticles (Ni-Co BMNPs) are synthesized and applied as an efficient catalyst in the chemoselective transfer hydrogenation of nitroarenes (CTH) using hydrazine hydrate as the hydrogen donor. The BMNPs can efficiently catalyze the reduction reaction without any additives under mild conditions with high TOF. Significantly higher activity is achieved when compared with corresponding single-component catalysts, optimal composition of the Ni-Co BMNPs was screened which was proved to be crucial in both the selectivity and yields. Excellent performance of Ni-Co BMNPs can be ascribed to the improved dispersion of active sites on the BMNPs surface (compared with Ni NPs) and the electron transfer from cobalt to nickel.
DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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Paragraph 0550-0551, (2014/01/08)
The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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Page/Page column 56, (2012/09/11)
The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
DIAMINOPYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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Page/Page column 50, (2012/09/11)
The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
