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Preparation method of ZD1839Form1 crystal form

A technology of zd1839form1 and crystal form, which is applied in the field of crystal form preparation of pharmaceutical compounds, can solve the problems of increasing operation steps and production cost, and achieve the effect of high purity, low cost and high yield

Inactive Publication Date: 2013-05-15
李彦
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  • Abstract
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  • Application Information

AI Technical Summary

Problems solved by technology

[0011] To obtain the ZD1839Form 1 crystal form, it is necessary to first prepare the solvate or the hydrate, and then use a solvent or a mixed solvent to wash out the solvate and then separate to obtain the ZD1839Form 1 crystal form. This method increases the operation steps , which increases production costs

Method used

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  • Preparation method of ZD1839Form1 crystal form
  • Preparation method of ZD1839Form1 crystal form
  • Preparation method of ZD1839Form1 crystal form

Examples

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Embodiment Construction

[0044] Example 1a, take 170 grams of ZD1839 pure product (purity 99%), add it to about 8 liters of acetone, heat and dissolve under stirring, and suction filter while it is hot to obtain a clear filtrate, crystallize under stirring for 16 hours, and precipitate solid crystals. The filter cake was obtained by filtration, dried at 50°C until constant weight, weighing: 145 g, yield 85%, melting point: 194.7-196.3°C. The crystal form of the product obtained is Form 1 type, see figure 1 . DSC melting point is 196.4℃ image 3 .

[0045] b. Take 10 grams of ZD1839 pure product (purity 99%), add it to 400 ml of acetonitrile, heat to dissolve under stirring, and suction filter while it is hot to obtain a clear filtrate, crystallize under stirring for 16 hours, precipitate solid crystals, filter to obtain filtrate Cake, dried to constant weight at 50°C, weighing: 9.1 g, yield 91%, melting point: 193.9-195.0°C.

[0046] c. Take 10 grams of ZD1839 pure product (purity 99%), add it to...

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Abstract

The invention relates to a preparation method of a ZD1839Form1 crystal form. The method comprises the following steps: dissolving the ZD1839 by using a solvent, stirring for separating out crystals; and filtering and drying the crystals, thereby obtaining the ZD1839Form1 crystal form, wherein the solvent for dissolving the ZD1839 can be a single solvent or a mixed solvent, and can also be a protonic solvent or an aprotic solvent.

Description

technical field [0001] The present invention relates to a method for preparing a crystal form of a medicinal compound, and more specifically relates to a method for preparing a ZD1839Form 1 crystal form. Background technique [0002] ZD1839 (English name Gefitinib, Iressa, ZD1839), chemical name N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholine-4-propoxy)quinazole Lin-4-amine, the structural formula is as follows, [0003] [0004] ZD1839 is a new type of small-molecular-weight tumor therapy drug, and its mechanism of action is mainly to block conduction by inhibiting EGFR autophosphorylation, inhibit tumor cell proliferation, and achieve targeted therapy. It is mainly used clinically for the treatment of locally advanced or metastatic non-small cell disease that has previously received chemotherapy lung cancer , especially for lung adenocarcinoma. [0005] ZD1839 was developed by AstraZeneca and launched in China in 2005. [0006] International patent application...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/94
Inventor 李彦
Owner 李彦
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