Complex compound of 5-hydroxy-1,3,6-trimethyluracyl with ambient acid, antidite activity and method of its production
SUBSTANCE: compound is produced by mixing succinic acid and 5-hydroxy-1,3,6-trimethyluracil in an equimolar amount in an organic solvent by heating the reaction mixture. Preferably, the process is carried out at a temperature of up to 40°C followed by cooling and filtration of the precipitated crystals. The compound is produced in 90% yield.
EFFECT: compound has antidote activity under conditions of exposure to toxic doses of poison - methaemoglobin-forming agent.
4 cl, 5 tbl, 3 ex
SUBSTANCE: invention relates to a novel complex of 5-hydroxy-6-methyluracil with 5-aminosalicylic acid of formula . The compound has anti-inflammatory activity and can be used as a basic active substance when producing novel medicinal preparations having anti-inflammatory action. The invention also relates to a method of obtaining said complex. The method includes reacting 5-hydroxy-6-methyluracil with 5-aminosalicylic acid in equimolar amounts in an aqueous medium at room temperature for 24 hours, followed by removal of water from the reaction mixture and obtaining the product.
EFFECT: wider range of pharmacological preparations with low toxicity, having higher anti-inflammatory activity.
2 cl, 1 tbl, 1 ex
SUBSTANCE: preparation shows an antitoxic activity, and can be used as an antidote for nitrite and nitrate poisoning. A complex compound of 5-hydroxy-6-methyluracil with ascorbic acid (5-hydroxy-6-methyluracil ascorbate) is described by formula: The preparation contains the complex compound in an amount of 0.3-0.4 wt %, and ascorbic acid - the rest. The method for producing the preparation consists in a reaction of 5-hydroxy-6-methyluracil and ascorbic acid taken in the relation of ascorbic acid: 5-hydroxy-6-methyluracil equal to 1:(0.0015-0.0022), in water as a solvent at a temperature of 20-40°C for 30-60 minutes. The complex compound is produced as shown by infra-red and NMR spectra. The antitoxic activity of 5-hydroxy-6-methyluracil on nitrite has been unknown before.
EFFECT: water removal from the reaction mixture under low pressure.
2 cl, 2 tbl, 1 ex
SUBSTANCE: invention relates to a novel complex of 5-hydroxy-6-methyluracil with sodium succinate (5-hydroxy-6-methyluracil succinate) of formula: , which exhibits antihypoxic activity. The disclosed compound widens the range of pharmacologically active compounds with low toxicity and high antihypoxic activity, which increase body resistance to certain types of hypoxia and in conditions influenced by other extreme environmental factors. The invention also relates to a method of producing the complex. The method involves mixing 5-hydroxy-6-methyluracil and sodium succinate in ratio of 1:10 in distilled water and then mixing the reaction mixture until dissolution of 5-hydroxy-6-methyluracil, removing the solvent from the reaction mixture and extracting the product.
EFFECT: output of the end product reaches 98%.
3 cl, 2 tbl, 4 ex
SUBSTANCE: invention refers to new biologically active high-immunotropic compound -N,N'-(sulphonyldi-1,4-phenylene)bis[(N",N'"-dimethyl)methyliminomethane]1,2,3,4-tetrahydro-6-methyl-2,4-dioxo-5-pyrimidinesulphonate of formula stated below to be used in treatment of, e.g., patients suffering from leprosy, allergic dermatosis, dermatitis herpetiformis. .
EFFECT: new compound is characterised with useful biological activity.
2 tbl, 1 ex
SUBSTANCE: invention relates to the new complex compound of 1,3-bis(2-hydroxyethyl)-5-hydroxy-6-methyluracil with fumaric acid of the formula which can be used in medicine as the substance capable of raising the survival rate in conditions under the influence of extreme environmental factors, particularly hypoxia. The new complex compound 1,3-bis(2-hydroxyethyl)-5-hydroxy-6-methyluracil with fumaric acid is obtained with 94% output by mixing equimolar quantities of 1,3-bis(2-hydroxyethyl)-5-hydroxy-6-methyluracil with fumaric acid in organic solvent with the subsequent heating of the reaction mixture for 2-3 hours, preferably at a temperature of 60-70°, removal of the solvent from the reaction mixture and the isolation of the product.
EFFECT: it makes it possible to increase the survival rate in harsh environmental conditions.
3 cl, 3 tbl, 5 ex
FIELD: organic chemistry, chemical technology.
SUBSTANCE: invention relates to the improved method for preparing 4,6-dimethoxy-2-(methylsulfonyl)-1,3-pyrimidine. Method involves reaction of 4,6-dichloro-2-(methylthio)-1,3-pyrimidine with alkaline metal methoxide in inert organic solvent, transfer of prepared 4,6-dimethoxy-2-(methylthio)-1,3-pyrimidine in aqueous acid medium and the following oxidation of this compound in the presence of catalyst if necessary, preferably, with an interphase catalyst, such as tricaprylmethylammonium chloride. Then method involves carrying out the purification stage wherein pH value of the aqueous acid reaction mixture is brought about to the value from 5 to 8 with aqueous base, such as alkaline metal hydroxide, for example, sodium hydroxide at temperature 10-90°C and stirring in the presence of absence of organic solvent, for example, aromatic hydrocarbon, such as benzene, toluene or isomeric xylenes, or alcohol, such as methanol or ethanol. Also, invention relates to using the prepared compound as an intermediate substance for synthesis of herbicide, in particular, 7-[(4,6-dimethoxypyrimidin-2-yl)thio]-3-methylphthalide by reaction of 7-mercapto-3-methylphthalide of compound in preparing herbicides, for example, 7-[(4,6-dimethoxypyrimidin-2-yl)thio]-3-methylphthalide.
EFFECT: improved preparing method.
24 cl, 2 sch, 1 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention relates to 4,4'-sulfonyl-bis-(N,N'-dimethylammoniomethyleneaniline)-chloride, 6-methyl-2,4-dioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonate of the formula (I) eliciting antibacterial, antimycobacterial and immunotropic activities. Also, invention describes a pharmaceutical composition based on compound of the formula (I).
EFFECT: valuable medicinal properties of compounds and composition.
3 cl, 7 tbl, 2 ex
FIELD: organic chemistry, biochemistry, pharmacy.
SUBSTANCE: invention relates to new heterocyclylsulfonyl alkylcarboxylic acids and their derivatives of the general formula (1): or their pharmaceutically acceptable salts, N-oxides or hydrates possessing the inhibitory effect on kinase activity and to the focused library for search of active leader-compounds comprising at least abovementioned compound. In the general formula 91) W represents optionally substituted heterocyclic radical, among them: pyrrole-3-yl, thiophene-2-yl, isooxazole-4-yl, pyrazole-4-yl, imidazole-4-yl, pyridine-3-yl, 1H-2,4-dioxopyrimidine-5-yl, 2,3-dihydro-1H-indole-5-yl, 2,3-dihydro-1H-indole-7-yl, 1,3-dihydro-2-oxoindole-5-yl, 2,3-dioxo-1H-indole-5-yl, 2-oxo-3H-benzoxazole-6-yl, benzothiazole-6-yl, 1H-benzimidazole-5-yl, benzo[1,2,5]oxadiazole-4-yl, benzo[1,2,5]thiadiazole-4-yl, 1,2,3,4-tetrahydroquinoline-6-yl, 3,4-dihydro-2-oxo-1H-quinoline-6-yl, quinoline-8-yl, 1,4-dihydro-2,3-dioxoquinoxaline-6-yl, 3-oxo-4H-benzo[1,4]oxazine-7-yl, 3-oxo-4H-benzo[1,4]thiazine-7-yl, 2,4-dioxo-1H-quinazoline-6-yl, 2,4-dioxo-1,5-dihydrobenzo[b][1,4]diazepine-7-yl or 2,5-dioxo-3,4-dihydrobenzo[b][1,4]diazepine-7-yl; Y represents optionally substituted methylene group; R1 represents chlorine atom, optionally substituted hydroxyl group, optionally substituted amino-group, optionally substituted azaheterocyclyl; n = 1, 2 or 3; or Yn represents carbon atom of optionally substituted (C3-C7)-cycloalkyl or optionally substituted (C4-C7)-heterocyclyl. Also, invention relates to a pharmaceutical composition in form of tablets, capsules or injections placed into pharmaceutically acceptable package.
EFFECT: valuable properties of compounds.
5 cl, 3 sch, 5 tbl, 6 ex
< / BR>where R denotes cyclopropyl, cyclobutyl, cyclohexyl, phenyl, unsubstituted or mono -, di - or tizamidine group selected from hydroxy, C1-C4of alkyl, C1-C4alkoxy, halogen, trifloromethyl, ceanography and amino groups; 1-or 2-naphthyl, 9-anthracene; 2-anthrachinone, Persil, unsubstituted or substituted group selected from1-C4of alkyl, C1-C4alkoxy, ceanography and halogen; 2-, 3 - or 4-chinoline, oxiranyl, 1-benzotriazolyl, 2-benzoxazolyl, furanyl, substituted C1-C4alkoxycarbonyl; C1-C4alkylsulphonyl or benzoyl; R1denotes halogen or1-C4alkyl, R2and R3independently represent hydrogen or C1-C4alkyl; X denotes an oxygen atom and Y represents an oxygen atom, a sulfur atom or a carbonyl, or their pharmaceutically acceptable salts, method of production thereof and pharmaceutical composition having antiviral activity, containing antiviruse-effective amount of compounds of General formula I
SUBSTANCE: method of producing calcium succinate is carried out by oxidising an organic substance with a peroxide in the presence of a catalyst, the organic substance used being furfurol and the peroxide being hydrogen peroxide. The process is carried out in the presence of vanadyl sulphate and calcium carbonate until the furfurol and peroxides are exhausted. Crystalline acidic calcium succinate is separated from the pre-filtered oxidate while cooling. The disclosed method aims to utilise industrially available reagents, including a safer oxidising agent and an affordable catalyst.
EFFECT: simple and cheaper process owing to use of industrially produced cheaper hydrogen peroxide and vanadium sulphate, safer process owing to use of hydrogen peroxide instead of sodium peroxide as the oxidising agent.
SUBSTANCE: aqueous ammonium salt solution is reacted with an organic extraction agent selected from a group comprising amines of general formula (0). R1, R2 and R3 are independently identical or different, branched or straight, optionally substituted hydrocarbon residues or a hydrogen atom H, and the salt is split at temperature and pressure at which the aqueous solution and the extraction agent are in liquid aggregate states. An auxiliary medium is added for stripping the carrier gas in order to remove NH3 from the aqueous solution, and a portion of the formed free organic acid is converted to the organic extraction agent. The organic acid is 2-hydroxyisobutyric acid and the extraction agent is dialkylamine. Freed ammonia is removed from the aqueous solution by a continuous gas stream and can be returned to the production process. The free acid can be extracted from the extraction agent using a method such as distillation, rectification, crystallisation, reverse extraction, chromatography, adsorption or by membrane methods.
EFFECT: cheap non-polluting method carried out without a salt load and which includes complete recovery through a closed cycle.
14 cl, 3 dwg, 8 ex
SUBSTANCE: invention relates to improved method of obtaining ammonium salts of fumaric or succinic acid, which are used for production of biologically active additives or medications, as well as in veterinary and food industry. Method lies in neutralisation of respective acid with neutralising compound in water medium, where as neutralising compound ammonium carbonate or bicarbonate is used, with molar stoichiometric or exceeding stoichiometry by 4-5% ratio of acid and ammonium carbonate or bicarbonate, neutralisation is carried out in saturated water solution of synthesised salt, at temperature not higher than 40°C, with further product separation and its drying at temperature not higher than 70°C. Method can be realised in conditions of industrial production. It is possible to obtain ecologically pure salts with content of main substance not lower than 99.0 wt %, and output not lower than 98%.
EFFECT: method makes it possible to increase output of target products and ensures their stably high quality due to obtaining them mainly in crystalline form.
4 cl, 5 ex
SUBSTANCE: strain Yarrowia lipolytica All-Russian collection of industrial microorganisms Y-3753 is proposed - producent of succinic acid. The strain may be produced on nutrient medium, containing glucose as the consumable carbon source, in absence of substances that stabilise pH, succinic acid in amount of up to 60 g/l of cultural fluid.
EFFECT: improved properties of the strain.
1 tbl, 1 ex
SUBSTANCE: invention refers to a method of producing succinic acid with using a Yarrowia lipolytica yeast strain, Russian National Collection of Industrial Microorganisms No. Y-3314. Said yeast is modified in such a manner that they have lowered succinate dehydrogenase activity. The method involves a stage of yeast strain incubation in a nutrient medium containing glycerine, and recovery of succinic acid from a culture fluid.
EFFECT: use of the Yarrowia lipolytica strain, Russian National Collection of Industrial Microorganisms No Y-3314 has ensured substantially increased yield of succinic acid in this method.
2 cl, 2 dwg, 5 tbl, 5 ex
SUBSTANCE: invention relates to a method of producing malonate or manganese (II) succinate, which can be used in different areas of chemical practice, in analytical control and scientific research, through direct reaction of a metal and its dioxide with carboxylic acid in the presence of an organic solvent and stimulating iodine additive in a vertical type bead mill with a high-speed mixer and glass beads as grinding medium, where manganese, its dioxide and carboxylic acid in the initial load are taken in molar ratio 1+x):1:(2+x) so as to obtain (2+x)m moles of salt, where x in the given molar ratio of reagents equals 0.4±0.1 for amber acid and 1.0±0.1 for malonic acid, and m is the number of moles of manganese dioxide in the load; iodine is taken in amount of 0.05 mol/kg of the reaction mixture after loading organic solvent and acid, but before loading manganese dioxide and metal. Total mass of acid, metal and its dioxide lies between 15 and 25% of the mass of the initial load, and ratio of mass of beads to mass of the load is 1:1. The process is started at room temperature and carried out under forced cooling conditions at temperature ranging from room temperature to 40°C while controlling by taking samples until exhaustion of all loaded reagents into the target salt, after which the process is stopped. The suspension of the final reaction mixture is separated from the beads and filtered. The product residue is washed with a liquid phase solvent and taken for purification from trace metal and its dioxide through recrystallisation, and the filtrate and washing solvent are returned to the repeated process.
EFFECT: process takes place at acceptable rates and ends with virtually complete consumption of all loaded reagents.
2 cl, 19 ex
FIELD: organic synthesis.
SUBSTANCE: invention concerns an improved method for synthesis of manganese(II) succinate tetrahydrate wherein manganese(II) carbonate is portionwise added to succinic acid aqueous solution at molar ratio 1:1:4.5, respectively, under continuous stirring and, while maintaining constant temperature 60-65°C, each subsequent portion being added after complete dissolution of preceding manganese carbonate portion, after which desired product is isolated via recrystallization. Method can be used under industrial-scale conditions.
EFFECT: improved purity of product and minimum reactants used.
3 dwg, 2 tbl, 5 ex
FIELD: organic chemistry, chemical technology.
SUBSTANCE: invention relates to improved method (variants) for conversion of maleic acid to 1,4-butanediol, gamma-butyrolactone and/or tetrahydrofuran. Method for synthesis for at least one of product chosen from a group comprising gamma-butyrolactone, 1,4-butanediol and tetrahydrofuran involves the following steps: creature of the first hydrogenation zone and the second hydrogenation zone that are bound successively; feeding to the first zone of a raw flow that comprises maleic acid; caring out reaction in the first hydrogenation zone of the parent maleic acid and hydrogen in contact with a catalyst to yield the reaction product comprising succinic acid; feeding to the second zone the hydrogenation product from the first hydrogenation zone; carrying out the hydrogenation reaction of the reaction product obtained in the first hydrogenation zone in the second hydrogenation zone in contact with a catalyst for preparing a product that comprises at least one product from a group comprising gamma-butyrolactone, 1,4-butanediol and tetrahydrofuran. Method involves control over temperature in first hydrogenation zone by manner that maleic acid temperature in the raw flow and temperature in the first hydrogenation zone doesn't exceed 120°C, and the reaction heat liberated in the first hydrogenation zone is used in enhancing the reaction product reaction above 130°C before feeding the reaction product from the first hydrogenation zone to the second hydrogenation zone resulting to minimal corrosion effect of maleic acid and enhancing time for working life of reactor and improving the complete effectiveness of the process.
EFFECT: improved method of synthesis.
13 cl, 1 ex
FIELD: production of calcium succinate useful in pharmacology, veterinary, medicine as drug or bioactive additive.
SUBSTANCE: calcium succinate in obtained by reaction of calcium chloride solution with reactive mixture of succinic acid and sodium hydroxide in molar ratio of 1:2, respectively at 20-30°C. Calcium chloride solution is added for 2 hours followed by mixture conditioning for 3 hours for crystallization finishing. Precipitate is separated, washed on filter and dried at 100°C for 12 hours. Target product is obtained in form of monohydrate.
EFFECT: accelerated method with reduced energy consumption.
FIELD: new 2,4,6-trimethyl-3-oxypyridine nitrosuccinate and method for production thereof.
SUBSTANCE: claimed compound is useful in medicine as future antiishemic agent with vasodilatation effect and has potent protective action in barotraumatic damages and ballistic wounds due to inhibition of secondary necrosis creation and progress. Compound of present invention is obtained by nitration of malic acid with mixture of sulfuric and nitric acids, separation of nitrohydroxymalic acid and treatment thereof with 2,4,6-trimethyl-3-oxypyridine in alcohol media with subsequent isolation of target product.
EFFECT: new antiishemic agent.
2 cl, 1 ex
SUBSTANCE: what is presented is a method for acute exposure to organophosphates with pronounced non-anticholinesterase mode of toxicity. A method consists in preventive administration of β-oestradiol 100 mg/kg 20-60 min prior to application of the toxic agent organophosphate.
EFFECT: reducing the manifestations of first signs of the exposure, developing convulsions and complete elimination of animals' death experimentally, administering β-oestradiol 5 days or 1 day before the exposure has not been producing such an effect.