- Preparation method for dasatinib monohydrate
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The invention provides a preparation method for a dasatinib monohydrate. The dasatinib monohydrate is obtained by a reaction of dasatinib in an ethanol aqueous solution. According to a technical scheme of the invention, the high-quality dasatinib monohydrate can be obtained; tedious separation and purification steps are avoided; operation is simple; the waste of raw materials is also avoided; theproduction cost is reduced; and the preparation method is more applicable to industrial production.
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Paragraph 0041; 0072-0073
(2020/07/13)
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- [...] a novel crystalline form of water composition and its preparation method and pharmaceutical composition
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The invention relates to the technical field of pharmaceuticals, and specifically relates to a novel crystal form of dasatinib monohydrate, and a preparation method and a pharmaceutical composition thereof. The novel crystal form of dasatinib monohydrate is very stable under conditions of illumination, high temperature, high humidity and accelerated experimentation conditions. The pharmaceutical composition has good dissolution rate, and is stable under a condition with a high temperature. Besides, compared with a conventional method, the preparation method provided by the invention has the advantages of simple operation and controllable quality. More importantly, the novel crystal form is relatively stable in a preparation process.
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Paragraph 0081-0104
(2018/04/20)
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- A convenient new and efficient commercial synthetic route for dasatinib (Sprycel)
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A new and efficient synthetic route for dual-Src/Abl kinase inhibitor dasatinib (Sprycel), an anticancer drug, is described. This commercially viable process yields dasatinib monohydrate free of potential impurities with consistent yield of 68% in route A and 61% in route B with HPLC purity >99.80% over four stages.
- Suresh, Garbapu,Nadh, Ratnakaram Venkata,Srinivasu, Navuluri,Yennity, Durgaprasad
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p. 1610 - 1621
(2017/09/08)
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- POLYMORPHS OF DASATINIB AND PROCESS FOR PREPARATION THEREOF
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Provided is dasatinib, solvates thereof and their crystalline forms, methods for their preparation, and pharmaceutical compositions thereof.
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Page/Page column 32-33
(2009/05/28)
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- ORAL ADMINISTRATION OF N-(2-CHLORO-6-METHYLPHENYL)-2-[[6-[4-(2-HYDROXYETHYL)-1-PIPERAZINYL]-2-METHYL-4-PYRIMIDINYL]AMINO]-1,3-THIAZOLE-5-CARBOXAMIDE AND SALTS THEREOF
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Disclosed are a method of treating cancer and/or other proliferative diseases comprising orally administering N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide or a salt thereof, and pharmaceutical compositions comprising N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide or a salt thereof. Also disclosed are N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)-1-piperazinyl)-2-methyl-4-pyrimidinyl)amino)-1,3-thiazole-5-carboxamide salts, as well as crystalline forms thereof.
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Page/Page column 57-58
(2010/11/26)
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- PROCESS FOR PREPARING 2-AMINOTHIAZOLE-5-AROMATIC CARBOXAMIDES AS KINASE INHIBITORS
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The invention relates to processes for preparing compounds having the formula (I) and crystalline forms thereof, wherein Ar is aryl or heteroaryl, L is an optional alkylene linker, and R2, R3, R4, and R5, are as defined in the specification herein, which compounds are useful as kinase inhibitors, in particular, inhibitors of protein tyrosine kinase and p38 kinase.
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Page/Page column 58-59
(2008/06/13)
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