FIELD: chemistry.
SUBSTANCE: invention relates to a method for the production of a polymorph of 4-(3-ethoxy-4-hydroxybenzyl)-N-(2,4-difluorphenyl)-5-oxo-5,6-dihydro-4H-1,3,4-thiadizine-2-carboxamide. The method is carried out by obtainment of a solution of a compound in tetrahydrofuran with a compound concentration of 1.1-1.3 g/ml at 60°C during mixing, then, the resulting solution is filtered through a filter heated to the same temperature to a receiver heated to the same temperature to obtain filtrate, and the resulting filtrate is cooled to 4°C to obtain crystals. Resulting crystals have primitive cubic syngony, characteristics peaks of high intensity are present in powder X-ray diagram, at angles 2θ equal to 14.9°±0.1°, 16.0°±0.1°, and 27.5°±0.1°, as well as characteristic peaks of medium intensity at angles 2θ equal to 18.3°±0.1° and 26.2°±0.1°. A melting point determined by differential scanning calorimetry is in the range from 99.7 to 101.8°C.
EFFECT: obtainment of a polymorph of 4-(3-ethoxy-4-hydroxybenzyl)-N-(2,4-difluorphenyl)-5-oxo-5,6-dihydro-4H-1,3,4-thiadizine-2-carboxamide with better characteristics, such as indicators of solubility, melting point, thermal stability.
1 cl, 6 dwg, 4 tbl, 2 ex
Title | Year | Author | Number |
---|---|---|---|
SOLID DISPERSION of 4- (3-ETHOXY-4-HYDROXIBENZIL) -5-OXO-5,6-DIHYDRO-4H- [1,3,4] -THIADIAZINE-2- (2,4-DIFLUOROPHENYL) -CARBOXAMIDE FOR PRODUCING PHARMACEUTICAL FORMULATION AND METHOD OF TREATMENT OF CHRONIC INFECTIOUS DISEASES | 2020 |
|
RU2743927C1 |
APPLICATION OF 4-(3-ETHOXY-4-HYDROXYBENZYL)-5-OXO-5,6-DIHYDRO-4H-[1,3,4]-THIADIAZINE-2-(2,4-DIFLUOROPHENYL)-CARBOXAMIDE TO SUPPRESS INFECTION, CAUSED BY ANTIBIOTIC-RESISTANT PSEUDOMONAS AERUGINOSA STRAINS, AND METHOD OF SUPPRESSION OF THIS INFECTION | 2016 |
|
RU2624846C1 |
PHARMACEUTICAL COMPOSITION OF 4-(3-ETHOXY-4-HYDROXYBENZYL)-5-OXO-5,6-DIHYDRO-4H-[1,3,4]-THIADIAZIN-2-(2,4-DIFLUOROPHENYL) CARBOXAMIDE IN CRYSTALLINE FORM , AND USE THEREOF AS ANTIBACTERIAL AGENT FOR TREATING ACUTE, RECURRENT AND CHRONIC INFECTIONS | 2020 |
|
RU2737087C1 |
PATHOGENIC BACTERIA-INHIBITING BIOLOGICALLY ACTIVE SUBSTANCES AND METHOD OF INHIBITING PATHOGENIC BACTERIA TYPE III SECRETION | 2010 |
|
RU2447066C2 |
NOVEL CRYSTALLINE FORM OF 5-CHLORO-N-({(5S)-2-OXO-3-[4-(5,6-DIHYDRO-4H-[1,2,4]TRIAZIN-1-YL)PHENYL]-1,3-OXAZOLIDIN-5-YL}METHYL)THIOPHENE-2-CARBOXAMIDE METHANESULPHONATE AND PHARMACEUTICAL COMPOSITION CONTAINING SAME | 2014 |
|
RU2663617C1 |
NEW CRYSTAL AND AMORPHOUS FORM OF TRYAZOL[4,5-d] PYRIMIDINE | 2001 |
|
RU2325391C2 |
NONHYGROSCOPIC CRYSTALLINE 5-[(Z)-(5-FLUORO-2-OXO-1,2-DIHYDRO-3H-INDOL-3-YLIDENE)METHYL]-N-[(2S)-2-HYDROXY-3-MORPHOLIN-4-YLPROPYL]-2,4-DIMETHYL-1H-PYRROL-3-CARBOXAMIDE MALEATE SALT, PHARMACEUTICAL COMPOSITION AND METHOD FOR CANCER TREATMENT | 2004 |
|
RU2319702C2 |
NOVEL CRYSTALLINE FORM OF TRIAZOLO(4,5-d)PYRIMIDINE | 2005 |
|
RU2418802C2 |
QUINAZOLIN-4-ONE DERIVATIVES USEFUL IN THE TREATMENT OF BRAF-ASSOCIATED DISEASES AND DISORDERS | 2020 |
|
RU2797606C1 |
BIOLOGICALLY ACTIVE SUBSTANCES SUPPRESSING PATHOGENIC BACTERIA, AND METHOD FOR INHIBITING TYPE III SECRETION IN PATHOGENIC BACTERIA | 2012 |
|
RU2495036C1 |
Authors
Dates
2022-12-05—Published
2022-10-06—Filed