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A new preparation method for Dasatinib N-6 crystal form

A crystal form and crystal technology, applied in the field of preparation of dasatinib N-6 crystal form, can solve the problems of cumbersome operation and inability to realize industrialized production, and achieve the effects of strong operability, low cost and strong controllability

Active Publication Date: 2012-08-22
JIANGSU SIMCERE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above method is to obtain the N-6 crystal form in water, and there is a risk of transforming into a stable crystal form H1-7 (monohydrate) during the scale-up process. In addition, the method is cumbersome to operate and cannot be industrialized.

Method used

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  • A new preparation method for Dasatinib N-6 crystal form
  • A new preparation method for Dasatinib N-6 crystal form
  • A new preparation method for Dasatinib N-6 crystal form

Examples

Experimental program
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Effect test

Embodiment 1

[0017] Embodiment 1: Preparation of Dasatinib N-6 crystal form

[0018] Weigh Dasatinib (487mg, 1mmol), then add it to the reaction flask, add 13mL methanol, control the temperature at 70°C, stir magnetically, slowly drop to 20°C after dissolving, filter, and wash with cold methanol (3×2mL) , dried under vacuum at 30°C to obtain 478 mg of Dasatinib N-6 crystal form, with a yield of 98%.

Embodiment 2

[0019] Embodiment 2: Preparation of Dasatinib N-6 crystal form

[0020] Weigh Dasatinib (487mg, 1mmol), then add it to the reaction flask, add 20mL methanol, control the temperature at 70°C, stir magnetically, slowly drop to 15°C after dissolving, filter, and wash with cold methanol (3×2mL) , dried under vacuum at 30°C to obtain 428 mg of Dasatinib N-6 crystal form, with a yield of 88%.

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Abstract

The invention provide a preparation method for Dasatinib N-6 crystal form, which dissolves the Dasatinib in the methanol and then cools and crystallizes to obtain the above Dasatinib N-6 crystal form.

Description

technical field [0001] The present invention relates to the technical field of preparation of polymorphic drugs, and more specifically relates to a preparation method of Dasatinib N-6 crystal form Background technique [0002] Dasatinib, also known as N-(2-chloro-6-methylphenyl)-2-{[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2 -Methyl-4-pyrimidinyl]amino}-5-thiazole carboxamide, its structural formula is as shown in formula 1, is the antineoplastic drug that U.S. Bristol-Myers Squibb company develops, and listed in the U.S. in February, 2006, trade name is Sprycel is clinically used for adults with various stages of chronic myeloid leukemia who have failed or are intolerant to previous treatment, and can also be used for the treatment of adult patients with Philadelphia chromosome-positive acute lymphoblastic leukemia who are resistant or intolerant to other therapies. [0003] [0004] According to relevant literature reports, in addition to pure crystal forms such as T1H1-7 ...

Claims

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Application Information

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IPC IPC(8): C07D417/12
Inventor 叶建胜黄常康李玲王青松杨攀吴鹤松
Owner JIANGSU SIMCERE PHARMA
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