Preparation method of tirofiban hydrochloride

A technology for tirofiban and hydrochloric acid, applied in the field of preparing tirofiban hydrochloride, can solve the problems of high potential safety hazard, potential safety hazard, troublesome solvent recovery and processing, etc., achieves low-carbon environmental protection reaction conditions, improves safety, The effect of simple salt-forming conditions

Active Publication Date: 2013-03-20
通辽市华邦药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This type of method has the following disadvantages: 1. A large amount of organic solvents are used in the salt-forming process, resulting in more or less organic solvents remaining in the finished product of tirofiban hydrochloride, which has certain potential safety hazards for clinical medication, especially the bulk drug It is used for injection; 2. Solvent recovery is troublesome, the cost increases, the production process is polluted, and the safety hazard is high

Method used

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  • Preparation method of tirofiban hydrochloride
  • Preparation method of tirofiban hydrochloride
  • Preparation method of tirofiban hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Weigh 220.0 g of tirofiban, add 4.4L of 1.2mol / L hydrochloric acid to the reaction vessel, heat to 80°C under stirring, to completely dissolve the tirofiban, and keep stirring for 30 minutes after dissolving. Add 2.2 g of activated carbon and stir at 80°C for 30 minutes to decolorize. Filtrate under reduced pressure while hot, cool to 18°C ​​with stirring, and maintain crystallization for 24 hours. The crystals were separated and washed with purified water to obtain a white solid, which was dried at 40-50°C to constant weight. The pulverized package can be directly used as the raw material for injection preparations.

Embodiment 2

[0020] Weigh 220.0 grams of tirofiban into the reaction bottle, add 6.6L of 0.5mol / L hydrochloric acid, and heat to 100±2°C under stirring to completely dissolve the tirofiban. After dissolving, keep stirring for 30 minute. Add 2.2 g of activated carbon for needles and stir at 100±2°C for 30 minutes to decolorize. Filtrate under reduced pressure while hot to another reaction flask. It was cooled to 30°C under stirring, and a large amount of solids precipitated out. Stir at 30°C±2°C for 24 hours. Filter under reduced pressure, wash with 200 mL of purified water, and repeat the washing 3 times to obtain a white solid. Spread the solid out and dry at 40-50°C until constant weight. The pulverized package can be directly used as the raw material for injection preparations.

Embodiment 3

[0022] Weigh 220.0 grams of tirofiban, and add 2.20L of 1.5mol / L hydrochloric acid to the reaction bottle, heat to 75±2°C under stirring to completely dissolve the tirofiban, and keep stirring for 30 minutes after dissolving. minute. Add 2.2 g of activated carbon for needles, and stir at 75±2°C for 30 minutes to decolorize. Filtrate to another reaction bottle under reduced pressure while hot, and cool to 0°C while stirring, a large amount of solids precipitate out. Stir at 0±2°C for 24 hours. Filter under reduced pressure, wash with 200 mL of purified water, and repeat the washing 3 times to obtain a white solid. Spread the solid out and dry at 40-50°C until constant weight. The pulverized package can be directly used as the raw material for injection preparations.

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PUM

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Abstract

The invention provides a preparation method of tirofiban hydrochloride. The preparation method has the advantages of simple salt forming conditions, low carbon and environmentally friendly characteristics, high product purity and no residue of organic solvents. The preparation method is characterized in that tirofiban is dissolved in 0.5 to 1.5 mol / L of a hydrochloric acid solution and based on the character that solubility of a tirofiban hydrochloride product in the hydrochloric acid solution can be influenced greatly by temperature variation, pure tirofiban hydrochloride crystals are obtained though cooling. The pure tirofiban hydrochloride crystals obtained by the preparation method have not only high purity but also no residue of organic solvents. Therefore, clinical medication safetyis improved obviously.

Description

Technical field: [0001] The invention relates to a method for preparing tirofiban hydrochloride. Background technique: [0002] The chemical name of tirofiban is "N-(n-butylsulfonyl)-O-[4-(4-piperidinyl)butyl]-L-tyrosine". Tirofiban has the following chemical structure [0003] [0004] The compound is a non-peptide reversible antagonist of platelet glycoprotein IIb / IIIa receptor, which has the pharmacological activity of blocking platelet cross-linking and platelet aggregation by preventing fibrinogen from binding to glycoprotein IIb / IIIa . Tirofiban can form a salt with hydrochloric acid to form a stable, water-soluble tirofiban hydrochloride, which is convenient to be prepared as an injection for intravenous injection. The chemical structure of tirofiban hydrochloride is as follows: [0005] [0006] Clinically, tirofiban hydrochloride is widely used to treat patients with unstable angina or non-Q wave myocardial infarction, prevent cardiac ischemic events, and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D211/22
Inventor 闫志刚张曦赜杨秀伟曹建英马向霞
Owner 通辽市华邦药业有限公司
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