FIELD: chemistry.
SUBSTANCE: invention relates to a process for the preparation of form B of the polymorph of compound A characterized by the presence of peaks in the powder X-ray pattern at approximately 6.4, 7.2, 19.3, 19.9, 21.6, 22.1 and 22.6°2θ obtained using radiation Cu Kα where the term "approximately" refers to the specified value of± 0.2 °2θ. The method includes the following steps: suspending compound A in chloroform at room temperature; or diffusion of anti-solvent vapor into a concentrated solution of compound A in either methanol or chloroform, where the anti-solvent is methyl tert-butyl ether (MTBE); cooling a solution of compound A in acetone, isopropyl acetate, 2-Me-THF, ethyl acetate, acetonitrile or a mixture of chloroform and heptane from 50 to 5°C or up to -20°C; or adding an anti-solvent to a solution of compound A in chloroform, methanol, acetone or acetonitrile, where the anti-solvent is isopropyl acetate (IPAc), toluene or isopropanol (IPA).
(A)
EFFECT: development of a method of obtaining form B of compound A polymorph with improved solubility, hygroscopicity and stability which can be used in medicine for the treatment of a disease in which Scr tyrosine kinase plays a role.
8 cl, 37 dwg, 14 tbl, 16 ex
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Authors
Dates
2023-09-05—Published
2018-09-07—Filed