2-ETHYL-6-METHYL-3-HYDROXYPYRIDINE OROTATE DIHYDRATE AND METHOD FOR PRODUCTION THEREOF Russian patent published in 2019 - IPC C07D213/65 C07D239/557 A61P9/00 A61P31/20 A61P1/16 A61P9/10 

Abstract RU 2690674 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel 2-ethyl-6-methyl-3-hydroxypyridine orotate dihydrate salt and a method for production thereof. 2-Ethyl-6-methyl-3-hydroxypyridine orotate dihydrate corresponds to formula C8H11NO⋅C5H4N2O4⋅2H2O. 2-Ethyl-6-methyl-3-hydroxypyridine orotate dihydrate can be used to produce a pharmaceutical composition for preventing and/or treating hypoxia, including 2-ethyl-6-methyl-3-hydroxypyridine orotate and a pharmaceutically acceptable carrier. Method of producing orotate involves A) 2-ethyl-6-methyl-3-hydroxypyridine (1000.0 mg) is dissolved in isopropyl alcohol (5 ml) at room temperature; B) orotic acid 56.9 mg (0.000364479 mol) is dissolved in 5 ml of a mixture of acetonitrile / water (1:1) at temperature of 80 °C; B) and adding 250 mcl of solution of 2-ethyl-6-methyl-3-hydroxypyridine (0.000364479 mole) obtained above; D) obtained mixture is cooled to room temperature naturally, precipitate is released 20–30 minutes after preparation. Product is obtained in form of a monocrystal. According to thermogravimetry and X-ray structural analysis, 2-ethyl-6-methyl-3-hydroxypyridine monochloride orotate dihydrate has an endothermic peak of 90–115 °C according to differential scanning calorimetry and peaks measurement data 2Θ° 8.1, 9.1, 10.0, 12.5, 12.9, 13.9, 15.2, 15.5, 18.0, 19.4, 19.6, 21.6, 22.1, 25.5, 28.7, 29.8, 30.4, 32.3 on X-ray diffraction measurements.

EFFECT: compound can be used as a antihypoxic agent for preventing or treating cardiovascular diseases, including atherosclerosis, myocardial dystrophy, anemia, IHD, including angina pectoris, myocardial infarction, chronic cardiac failure and heart rhythm disturbances, including magnesium-dependent arrhythmia, atrial fibrillation, or as an adjunct to liver diseases, including hepatitis, hepatosis and bile ducts caused by acute and chronic intoxication, except for organic damages of liver and bile ducts.

8 cl, 6 dwg, 1 ex

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RU 2 690 674 C2

Authors

Boldyrev Andrej Nikolaevich

Oblezov Aleksandr Evgenevich

Kazej Vasilij Igorevich

Dates

2019-06-05Published

2017-05-04Filed