CRYSTAL FORM OF PARP-1 INHIBITOR AND ITS PRODUCTION METHOD Russian patent published in 2023 - IPC C07D487/04 

FIELD: medicine.

SUBSTANCE: invention relates to a method for the production of a crystal form A of a compound of the formula I, where on a powder X-ray diffractogram obtained using Cu-Kα-radiation, characteristic peaks are presented with values of a diffraction angle 2θ of 9.58, 15.25, 17.09, 18.63, 21.11, 22.79, 23.99, 24.23, 27.26, 28.97. In this case, the method includes: (a) addition of 4-[[3-[[2-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[1,5-α]pyrazine-7-yl]carbonyl]-4-fluorophenyl]methyl-1(2H)-phthalazinone (formula I) to a solvent (I), dissolution, filtration, concentration to a dry state, where the solvent (I) is butanone; (b) addition of a solvent (II), dissolution of the above-mentioned solid substance by mixing or heating, and mixing with crystallization, or addition of a solvent (II), heating with a reverse refrigerator with shaking, mixing, and cooling; (c) filtration to obtain crystals of the compound of the formula I. At the same time, the solvent (II) is selected from butanone, tetrahydrofuran, acetone, methanol, ethanol, tetrahydrofuran/water, acetone/water, acetonitrile, acetonitrile/water, ethylacetate, and butanone/water.

EFFECT: method for the production of a crystal form A of a compound of the formula I, which is stable and can be used in medicine to obtain drugs inhibiting PARP-1, is developed.

5 cl, 5 dwg, 2 tbl, 14 ex