Dasatinib polycrystalline form medicament and preparation method thereof

Abstract

The invention provides a new dasatinib polycrystalline form medicament and a preparation method thereof. In a powder diffraction spectrum of a dasatinib polycrystalline form matter III provided by the invention, diffraction peaks exist at 2 theta of 6.2 plus or minus 0.2, 12.0 plus or minus 0.2, 15.3 plus or minus 0.2 and 18.4 plus or minus 0.2. The crystal form prepared by the preparation method provided by the invention has good chemical stability and high purity. The preparation method has the advantages of mild process conditions, simplicity in operation, stable and controllable quality and high yield, and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a dasatinib polymorphic form III and a preparation method thereof. Background technique [0002] Dasatinib, trade name Sprycel, is a tyrosine kinase inhibitor developed by Bristol-Myers Squibb. Adult patients of all stages of chronic myeloid leukemia who are resistant or intolerant to treatment regimens including imatinib mesylate. It can also be used to treat adult patients with Philadelphia chromosome-positive acute lymphoblastic leukemia who are resistant or intolerant to previous treatments. In February 2006, FDA approved the listing. The chemical name of dasatinib is N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl-2-methyl- 4-pyrimidinyl [amino]-5-thiazole carboxamide. The structure is as follows: [0003] [0004] The currently authorized and applied dasatinib crystal form patents are CN200580011916.6 (authorized), which discloses 5 crystal forms includin...

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Problems solved by technology

[0008] The above-mentioned prior art has the following deficiencies: (1) The preparation process is relatively cumbersome and there are many temperature control points; (2) A certain amount of seed crystals need to be added in the crystallization process, and the instructions emphasize that "seed crystals are not important for obtaining monohydrate Unnecessary, but better control of crystallization

[0013] There are many defects in the above-mentioned prior art: (1) The stability of the crystal form of dasatinib is poor; (2) The preparation method uses organic solvents to dry naturally for a long time; (3) The natural air-drying of a large amount of solvents has high requirements for the production environment The operator is very harmful; (4) The waste residue is not suitable for disposal, and there are potential safety hazards; (5) The preparation process is cumbersome; (6) It is not suitable for industrial production

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