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Faropenem sodium crystallization and preparation method thereof

A technology for the crystallization of faropenem sodium, which is applied in the field of β-lactam antibiotic faropenem sodium crystallization and its preparation, can solve the problems of thermal instability, uneconomical, discoloration, etc., and achieve the effect of excellent stability and reliable quality

Active Publication Date: 2007-09-12
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Faropenem sodium has poor stability during storage, and changes such as discoloration and decrease in purity will occur, and due to its physical and chemical properties, it will not only affect the stability of the preparation, but also make the preparation process difficult
Because β-lactam antibiotics have poor stability in aqueous solution and are unstable to heat, they cannot obtain relatively pure products by heating and distilling off water. The preparation of faropenem sodium in the existing literature is all obtained by freeze-drying in aqueous solution. Expensive freeze-drying equipment consumes a lot of energy in industrial production and cannot effectively purify the product. Generally, purification needs to be adsorbed and eluted by macroporous resins, which is time-consuming and uneconomical

Method used

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  • Faropenem sodium crystallization and preparation method thereof
  • Faropenem sodium crystallization and preparation method thereof
  • Faropenem sodium crystallization and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0046] Dissolve 10 g of crude faropenem sodium in 20 ml of distilled water, cool in an ice bath to 0°C, slowly add 60 ml of ethanol while stirring, keep stirring at this temperature for 1 hour, remove the ice bath, continue stirring overnight, and recover crystals, 40 After drying at ℃, 8.6 g was obtained, with a yield of 86%.

Embodiment 1

[0048] Dissolve 10 g of crude faropenem sodium in 10 ml of distilled water, cool in an ice bath to 4°C, slowly add 40 ml of acetone while stirring, keep stirring at this temperature for 0.5 hours, remove the ice bath, continue stirring overnight, and recover crystals, 40 ℃ drying to obtain 9.6g, yield 96%.

[0049] Example 2

[0050] Dissolve 10 g of crude faropenem sodium in 20 ml of distilled water, cool to 0°C with an ice bath, slowly add 30 ml of methyl ethyl ketone under stirring, keep stirring at this temperature for 1 hour, remove the ice bath, continue stirring overnight, and recover crystals, 40 ℃ drying to obtain 9.2g, yield 92%.

Embodiment 3

[0052] The yield and quality comparison of 4 embodiment gained products are shown in Table 1.

[0053] Example

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Abstract

This invention relates to the crystallization of compounds, specifically involving beta-lactam antibiotics faropenem Na crystallization and its preparation method.

Description

technical field [0001] The invention relates to the crystal form of the compound, in particular to the β-lactam antibiotic faropenem sodium crystal and a preparation method thereof. Background technique [0002] Faropenem sodium is a penem antibiotic developed by Suntory Company of Japan. It is similar to several carbapenem antibiotics that have been on the market. It has a broad antibacterial spectrum, strong antibacterial activity, and is stable to β-lactamase. Spectrum β-lactamase-producing bacteria, Citrobacter, Enterococcus and anaerobic bacteria also have good effects and other characteristics. It can be taken orally or injected, and can effectively inhibit a wide range of Gram-positive, negative and anaerobic bacteria. It is the most effective anti-anaerobic β-lactam antibiotic. Its chemical name is: (5R, 6S)-6-[(1R)-1-hydroxyethyl]-7-oxo-3-[(2R)-2-tetrahydrofuryl]-4-thio-1- Azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid sodium salt, which is usually a hydrate with 2...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/893C07D499/04A61P31/04
Inventor 张喜全张爱明
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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