NOVEL CRYSTALLINE FORMS OF 1-(4-{[6-AMINO-5-(4-PHENOXY-PHENYL)-PYRIMIDIN-4-YLAMINO]-METHYL}-4-FLUORO-PIPERIDIN-1-YL)-PROPENONE, SALT FORMS THEREOF, AND METHOD OF OBTAINING THEREOF Russian patent published in 2025 - IPC C07D401/12 A61K31/506 A61P35/00 A61P37/00 

Abstract RU 2836584 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing a crystalline anhydrous solid form of compound 1, which is form A1, characterized by four or more 2θ RPD peaks at 17.1 ± 0.2°, 17.4 ± 0.2°, 18.8 ± 0.2°, 20.0 ± 0.2° and 21.1 ± 0.2°, which involves dissolving compound 1 in an organic solvent between about 20 °C and 75 °C. Solvents are ethanol, 1-propanol, 2-propanol, 2-butanol, acetone, methyl ethyl ketone, methyl isobutyl ketone, ethyl acetate, 1,4-dioxane, diethyl ether, methyl tert-butyl ether, tetrahydrofuran, acetonitrile, dichloromethane, chloroform, toluene or pyridine, 1-butanol, iso-butanol, N,N-dimethylformamide, ortho-xylene, para-xylene or a mixture thereof, when dissolving compound 1 at 50 °C.

EFFECT: crystalline form of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-4-fluoro-piperidin-1-yl)-propenone (compound 1), having good crystallinity, easy hygroscopicity, high thermal stability.

6 cl, 57 dwg, 7 ex

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RU 2 836 584 C2

Authors

Lange Michael

Kuehn Clemens

Schlueter Tobias

Mederski Werner

Maillard David

Burini Edoardo

Dates

2025-03-18Published

2019-06-17Filed