- Preparation method of 3, 5-dichloroo-phenylenediamine
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The invention relates to an industrial preparation method of 3, 5-dichloroo-phenylenediamine, which comprises the following steps of: by using 3, 5-dichloroaniline as an initial raw material, carryingout protection, nitrification, deprotection and reduction reaction to synthesize the 3, 5-dichloroo-phenylenediamine. The 3, 5-dichloroo-phenylenediamine obtained in the process is a brown solid, thepurity is 97.5%, the conversion rate of raw materials in each step reaches 100%, the total yield of the whole process reaches 52.7%, 3, 5-dichloroaniline is used as an initial raw material, the positioning property is good, the impurity is few, and the purification is easy.
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- As neuroprotective agents of pharmaceutical compounds
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The invention discloses a medicinal compound as a neuroprotective agent. The medicinal compound is a neuronal nitric oxide synthase-postsynaptic density protein 95 (nNOS-PSD95) decoupling agent. The medicinal compound is a benzene ring derivative shown in the general formula (I) or its pharmaceutically acceptable salt. The invention further discloses a preparation method of the medicinal compound and a use of the medicinal compound in prevention and treatment on neuronal damage influence-caused diseases.
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Paragraph 0642; 0643; 0646; 0647
(2019/06/26)
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- Highly selective hydrogenation of aromatic chloronitro compounds to aromatic chloroamines with ionic-liquid-like copolymer stabilized platinum nanocatalysts in ionic liquids
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Platinum nanoparticles (PtNPs stabilized by an ionic-liquid-like-copolymer (IP) immobilized in various ionic liquids (ILs)) effectively catalyze the selective hydrogenation of aromatic chloronitro compounds to aromatic chloroamines, a reaction of considerable commercial significance. The preparation of 2,4-dichloro-3-aminophenol (DAP) has been primarily studied due to its important industrial applications. DAP is usually prepared from 2,4-dichloro-3-nitrophenol (DNP) by reduction with hydrogen using Ni- or Pt-based catalysts. Compared to reactions in molecular (organic) solvents, the ILs system provides superior selectivity with functionalized ILs containing an alcohol group demonstrating the best recyclability, and ultimately achieving a turnover number of 2025 which is 750 fold higher than Raney nickel catalyst. A universal catalyst-ionic liquid system for the conversion of aromatic chloronitro compounds to aromatic chloroamines was also established. TEM, XPS, IR spectroscopy were used to characterize the morphology of the nanocatalysts allowing their structure to be correlated to their activity.
- Yuan, Xiao,Yan, Ning,Xiao, Chaoxian,Li, Changning,Fei, Zhaofu,Cai, Zhipeng,Kou, Yuan,Dyson, Paul J.
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experimental part
p. 228 - 233
(2011/03/17)
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- Design, synthesis, and antiviral evaluation of 2-substituted 4,5- dichloro- and 4,6-dichloro-1-β-D-ribofuranosylbenzimidazoles as potential agents for human cytomegalovirus infections
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The syntheses of 2,4,6-trichlorobenzimidazole (4a) and 2-bromo-4,6- dichlorobenzimidazole (4b) were accomplished via the 2-amino intermediate (3) using a mild diazotization procedure. Ribosylation of 4a and 4b and subsequent deprotection afforded the corr
- Zou, Ruiming,Drach, John C.,Townsend, Leroy B.
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p. 802 - 810
(2007/10/03)
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- Glycine receptor antagonists and the use thereof
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Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia and treating psychosis are disclosed by administering to an animal in need of such treatment a compound having high affinity for the glycine binding site, lacking PCP side effects and which crosses the blood brain barrier of the animal. Also disclosed are novel 1,4-dihydroquinoxaline-2,3-diones, and pharmaceutical compositions thereof. Also disclosed are highly soluble ammonium salts of 1,4-dihydroquinoxaline-2,3-diones.
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- Synthesis and structure-activity relationships of substituted 1,4- dihydroquinoxaline-2,3-diones: Antagonists of N-methyl-D-aspartate (NMDA) receptor glycine sites and non-NMDA glutamate receptors
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A series of mono-, di-, tri-, and tetrasubstituted 1,4- dihydroquinoxaline-2,3-diones (QXs) were synthesized and evaluated as antagonists at N-methyl-D-aspartate (NMDA)/glycine sites and α-amino-3- hydroxy-5-methylisoxazole-4-propionic acid-preferring non-NMDA receptors. Antagonist potencies were measured by electrical assays in Xenopus oocytes expressing rat whole brain poly(A)+ RNA. Trisubstituted QXs 17a (ACEA 1021), 17b (ACEA 1031), 24a, and 27, containing a nitro group in the 5 position and halogen in the 6 and 7 positions, displayed high potency (K(b) ~ 6-8 nM) at the glycine site, moderate potency at non-NMDA receptors (K(b) = 0.9-1.5 μM), and the highest (120-250-fold) selectivity in favor of glycine site antagonism over non-NMDA receptors. Tetrasubstituted QXs 17d,e were more than 100-fold weaker glycine site antagonists than the corresponding trisubstituted QXs with F being better tolerated than Cl as a substituent at the 8 position. Di- and monosubstituted QXs showed progressively weaker antagonism compared to trisubstituted analogues. For example, removal of the 5-nitro group of 17a results in a ~100-fold decrease in potency (10a,b,z), while removal of both halogens from 17a results in a ~3000-fold decrease in potency (10v). In terms of steady-state inhibition, most QX substitution patterns favor antagonism at NMDA/glycine sites over antagonism at non-NMDA receptors. Among the QXs tested, only 17i was slightly selective for non- NMDA receptors.
- Keana,Kher,Sui Xiong Cai,Dinsmore,Glenn,Guastella,Huang,Ilyin,Lu,Mouser,Woodward,Weber
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p. 4367 - 4379
(2007/10/02)
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- Novel benzimidazoles as ligands for the strychnine-insensitive N-methyl-D-aspartate-linked glycine receptor
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Two new benzimidazole derivatives were synthesized and evaluated for their ability to inhibit the binding at the strychnine-intensivite N-methyl-D-aspartate(NMDA)-linked glycine receptor.The most potent one, the 4,6-dichlorobenzimidazole-2-carboxylic acid
- Louvet, P.,Lallement, G.,Pernot-Marino, I.,Luu-Duc, C.,Blanchet, G.
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- Quinoxaline-2,3-dione compounds and their preparation and use
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1-carboxyalkylquinoxaline-2,3(1H,4H)-dione compounds or tautomeric forms thereof of the formula STR1 wherein R represents hydrogen, C 1-6 -alkyl, including branched chains, or aralkyl and n represents the number from 0 to 5;R 4 represents hydrogen or hydr
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- Process for the manufacture of benzimidazolones-(2)
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Process for the manufacture of benzimidazolones-(2) wherein an o-phenylenediamine is reacted with optionally alkylated urea in the ratio of 1 to 1.3 moles per mole o-phenylenediamine in an organic solvent which has a solubility in water of not more than 5 g/l and has a boiling point above 100° C, at a temperature between 100° and 200° C.
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