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New preparation method for crystal form Gefitinib Form 1

A technology of crystal form and ethanol, applied in the field of polymorphic drug preparation, can solve the problems of increased operating cost, uncontrollability, hidden dangers in process amplification, etc., and achieves low cost, good crystallinity of crystal form, increased controllability and The effect of stability

Active Publication Date: 2011-02-16
HAINAN SIMCERE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In CN101177415A, the preparation method of Gefitinib Form1 crystal form is involved, but the method described is all obtained by beating DMSO solvate (Form 3) and MeOH solvate (Form 2) by other solvents, and the method is obtained in the process of process amplification There are hidden dangers and uncontrollability. In addition, the preparation process needs to obtain the solvate first and then obtain the Form 1 crystal form, which greatly increases the operating cost

Method used

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  • New preparation method for crystal form Gefitinib Form 1
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  • New preparation method for crystal form Gefitinib Form 1

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Embodiment 1: Preparation of Gefitinib Form 1 crystal form

[0024] Weigh Gefitinib (1g), then add it to a reaction flask, add 20mL of ethanol, control the temperature at 75°C, stir magnetically, slowly cool down to room temperature after dissolving, filter, wash with cold ethanol (3×1mL), and wash at 40°C After vacuum drying, 900 mg of Gefitinib Form I crystal form was obtained with a yield of 90%.

Embodiment 2

[0025] Embodiment 2: Preparation of Gefitinib Form 1 crystal form

[0026] Weigh Gefitinib (1g), then add it to the reaction flask, add 30mL isopropanol, control the temperature at 75°C, stir magnetically, slowly cool down to room temperature after dissolving, filter, and use cold isopropanol (3×1mL) After washing and vacuum drying at 40°C, 940 mg of Gefitinib Form I was obtained with a yield of 94%.

Embodiment 3

[0027] Embodiment 3: Preparation of Gefitinib Form 1 crystal form

[0028] Weigh Gefitinib (1g), then add it to the reaction flask, add 20mL n-butanol, control the temperature at 75°C, stir magnetically, slowly cool down to room temperature after dissolving, filter, and use cold n-butanol (3×1mL) After washing and vacuum drying at 40°C, 890mg of Gefitinib Form I was obtained with a yield of 89%.

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Abstract

The invention provides a new preparation method for a crystal form Gefitinib Form 1, which comprises the following steps: dissolving Gefitinib into one type or multiple types of solvents of ethanol, isopropanol and butyl alcohol; cooling; and crystallizing to prepare the crystal form Gefitinib Form 1.

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 GefitinibForm I crystal form Background technique [0002] Gefitinib, also known as N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]-4-quinazolinamine, its The structural formula is shown in Formula 1. It is an oral epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor developed by AstraZeneca Corporation of the United States. It was first listed in Japan in 2002 and entered China in 2005. The trade name is Iressa. It is used clinically for the treatment of Locally advanced or metastatic non-small cell lung cancer (NSCLC) who have previously received platinum-based antineoplastic drugs and docetaxel chemotherapy ineffective or not suitable for chemotherapy. [0003] [0004] Formula 1 [0005] WO9633980 mentions the purification of Gefitinib by methanol recrystallization,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D239/94
Inventor 叶建胜黄常康
Owner HAINAN SIMCERE PHARMA CO LTD
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