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New crystal of Dasatinib monohydrate and preparation method thereof

A technology of monohydrate and dasatinib, applied in the preparation method and pharmaceutical composition thereof, in the field of crystal form III of dasatinib monohydrate, which can solve the problems of difficult crystal quality and difficult to handle organic waste liquid, and achieve Easy operation, high crystal purity and good process repeatability

Active Publication Date: 2013-04-24
PHARMA RES INST OF BENCAO TIANYUAN OF BEIJING
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Obviously, it is difficult to control the quality of crystals obtained under such a complex system, and industrial production will bring a large amount of organic waste liquid that is difficult to handle, which will bring great pressure to environmental protection

Method used

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  • New crystal of Dasatinib monohydrate and preparation method thereof
  • New crystal of Dasatinib monohydrate and preparation method thereof
  • New crystal of Dasatinib monohydrate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Preparation of dasatinib monohydrate crystal form III

[0057] Take 28g of dasatinib and add it to 2000ml of methanol, stir and heat until dissolved, filter it once while it is hot, add 1400ml of water to the filtrate while stirring, stop stirring, let the temperature drop naturally, slowly precipitate fine crystals, and then add it under stirring at room temperature after 3 hours 600ml of water, stop stirring after adding, leave to crystallize. The precipitated white crystals were filtered by suction, washed with a small amount of methanol, dried under vacuum at 60°C, and assisted by phosphorus pentoxide to obtain 23 g of the product as a white crystalline powder.

Embodiment 2

[0059] Preparation of dasatinib monohydrate crystal form III

[0060] Take 10g of Dasatinib and add it to 1000ml of acetone, stir and heat to reflux to dissolve, filter once while it is hot, add 500ml of water to the filtrate while stirring, stop stirring, cool down naturally, slowly precipitate fine crystals, and stir again at room temperature after 4 hours. Add 500ml of water, stop stirring after adding, and leave to crystallize. The precipitated white crystals were filtered by suction, washed with a small amount, and dried under vacuum at 60° C., assisted by phosphorus pentoxide to obtain 8.4 g of the product as a white crystalline powder.

Embodiment 3

[0062] Preparation of dasatinib monohydrate crystal form III

[0063] Take 10g of Dasatinib and add it to 50ml of dimethylformamide, heat it to 70°C under stirring to dissolve, filter once while it is hot, add 75ml of water to the filtrate while stirring, stop stirring, and cool down naturally until fine crystals are slowly precipitated, at room temperature Add 30ml of water under stirring, stop stirring after adding, and leave to crystallize. The precipitated white crystals were filtered by suction, washed with a small amount, and dried under vacuum at 60° C., assisted by phosphorus pentoxide to obtain 7.3 g of the product as a white crystalline powder.

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PUM

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Abstract

The invention relates to the technical field of medicines, in particular to a crystal III of Dasatinib monohydrate, its preparation method and pharmaceutical composition. The crystal III of Dasatinib monohydrate provided in the invention is very stable under the conditions of illumination, high temperature, high humidity and accelerated testing. The pharmaceutical composition of crystal III of Dasatinib monohydrate has good dissolubility, and can be stable under high temperature conditions. In addition, compared with prior art, the preparation method provided in the invention has the advantages of simple operation and controllable quality.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to the crystal form III of dasatinib monohydrate, a preparation method and a pharmaceutical composition thereof. Background technique [0002] Dasatinib monohydrate, molecular formula C 22 h 26 ClN 7 o 2 S.H2O, molecular weight 506.02, CAS863127-77-9. The product name is SPRYCEL, which is an oral tyrosine kinase inhibitor developed by BMS, which is used for adult chronic myelogenous leukemia (CML), and can also be used for the treatment of Philadelphia chromosome-positive acute lymphoblastic leukemia and other diseases. Its chemical name is N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4- Pyrimidinyl]amino]-5-thiazolecarboxamide, the chemical structure is as follows: [0003] [0004] Chinese patent CN200580011916.6 (hereinafter referred to as "916") documents a crystalline form of dasatinib monohydrate and two crystalline forms of solvates...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12A61K31/506A61P35/00A61P35/02
Inventor 徐春霞孙学伟顾群李志刚
Owner PHARMA RES INST OF BENCAO TIANYUAN OF BEIJING
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