A kind of preparation method of gefitinib form 1 crystal form

A technology of gefitinib and crystal form, which is applied in the field of crystal form preparation of pharmaceutical compounds, can solve problems such as changes in dissolution rate and bioavailability of active compounds, unfavorable product quality, etc., and achieve the goal of avoiding dissolution rate and bioavailability change, benefit quality control, and improve stability

Active Publication Date: 2017-05-10
JIANGSU TASLY DIYI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If these different crystal forms exist, due to the different characteristics of the crystal forms, the dissolution rate and bioavailability of the active compound may change, which is not conducive to the control of product quality

Method used

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  • A kind of preparation method of gefitinib form 1 crystal form
  • A kind of preparation method of gefitinib form 1 crystal form
  • A kind of preparation method of gefitinib form 1 crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052]Add 1g of gefitinib into 20ml of acetone, control the temperature at 60°C, stir to dissolve all, and slowly cool down to room temperature after dissolving, collect the solid by filtration, wash with cold acetone (3×5mL), and dry in vacuum. According to X-ray diffraction analysis, it is Form1 crystal form of gefitinib. A total of 900 mg of Form1 crystal form of gefitinib was obtained, with a yield of 90%.

Embodiment 2

[0054] Add 1g of gefitinib into 20ml of 2-butanone, control the temperature at 70°C, stir to dissolve all, slowly cool down to room temperature after dissolving, collect the solid by filtration, wash with cold 2-butanone (3×5mL), vacuum After drying, the obtained crystals were analyzed by X-ray diffraction to be Form 1 crystal form of gefitinib. A total of 920 mg of Form 1 crystal form of gefitinib was obtained, with a yield of 92%.

Embodiment 3

[0056] Add 1g of gefitinib into 10ml of 2-pentanone, control the temperature at 90°C, stir to dissolve it all, slowly cool down to room temperature after dissolving, collect the solid by filtration, wash with cold 2-pentanone (3×5mL), vacuum After drying, the obtained crystals were analyzed by X-ray diffraction to be Form 1 crystal form of gefitinib. A total of 960 mg of Form1 crystal form of gefitinib was obtained, with a yield of 96%.

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Abstract

The invention provides a method for preparing a gefitinib Form I crystal form. Gefitinib is heated and dissolved into solvents such as acetone, and then cooled and crystallized, so as to obtain the gefitinib Form I crystal form.

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 Form1 crystal form of gefitinib. Background technique [0002] Gefitinib (English name: gefitinib), chemical name N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholine-4-propoxy)quinazole Lin-4-amine, whose structure is shown in formula-1, is a selective epidermal growth factor receptor (EGFR) protein tyrosine kinase inhibitor developed by AstraZeneca. The trade name of gefitinib is Iressa, which was first launched in Japan in July 2002 for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) who have previously received chemotherapy. In May 2003, it was approved by the FDA to go on the market in the United States, and in February 2005 it was approved by the SFDA to go on the market in China. [0003] [0004] International patent application WO2003072108 discloses f...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D239/94
CPCC07D239/94
Inventor 钟俊王国成
Owner JIANGSU TASLY DIYI PHARMA CO LTD
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