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Novel crystal form of biapenem and synthetic method thereof

A crystal form ratio and crystallization technology, applied in organic chemistry, antibacterial drugs, etc., can solve unclear problems

Inactive Publication Date: 2013-11-13
HARBIN PHARMA GRP CO LTD GENERAL PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Even if a single crystalline form is formed by chance, it is not clear how extraction can be performed to obtain a defined form

Method used

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  • Novel crystal form of biapenem and synthetic method thereof
  • Novel crystal form of biapenem and synthetic method thereof
  • Novel crystal form of biapenem and synthetic method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1: Preparation of Biapenem Form I

[0041] Add 300ml of water into the dissolution reaction bottle, control the temperature at 20°C, add 10g of crude biapenem under stirring, add 1g of activated carbon after dissolution, control the temperature at 40°C, stir for 20 minutes, filter, and transfer the filtrate to the crystallization reaction bottle , add 800ml crystallization solvent acetone and 0.1g seed crystal to the crystallization reaction bottle under stirring for crystallization, after the crystallization solvent is added, slowly cool down to 20°C, continue to stir and grow crystals for 2 hours, filter, wash with 80ml acetone, and drain Vacuum drying was carried out to obtain 9.20 g of biapenem crystals. (Yield 92.0%).

[0042] This crystal is used as a sample, and powder X-ray diffraction (hereinafter referred to as XRD) is measured to obtain figure 1 The X-ray diffraction pattern shown. From this result, it can be seen that X-ray diffraction peaks ap...

Embodiment 2

[0047] Example 2: Preparation of Biapenem II Crystal Form

[0048] Add 500ml of water into the dissolution reaction bottle, control the temperature at 20°C, add 10g of crude biapenem under stirring, add 1g of activated carbon after dissolution, control the temperature at 20°C, stir for 20 minutes, filter, and transfer the filtrate to the crystallization reaction bottle , add 1500ml of crystallization solvent methanol to the crystallization reaction bottle under stirring for crystallization. After the crystallization solvent is added, the temperature is controlled at 10°C, and the crystal is grown for 2 hours, filtered, washed with 80ml of methanol, and the product is vacuum-dried after pumping dry 9.11 grams of biapenem crystals. (Yield 91.1%).

[0049] This crystal is used as a sample, and powder X-ray diffraction (hereinafter referred to as XRD) is measured to obtain figure 1 The X-ray diffraction pattern shown. It can be seen from the results that X-ray diffraction pe...

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Abstract

The invention relates to crystal form I of (1R,5S,6S)-2-[(6,7-dihydro-5H-pyrazolo[1,2-alpha]-[1,2,4]triazole-hexabase)]sulfur-6R-1-hydroxyethyl]-1-methyl-carbapenem-3-carboxylate (biapenem), a preparation method of crystal form I, and a pharmaceutical composition containing the crystal form I of biapenem and one or more pharmaceutically acceptable carriers, excipients or diluents. Formula (I) is as described in the specification.

Description

technical field [0001] The invention relates to a new crystalline form I of biapenem, a synthesis method thereof, and a pharmaceutical composition containing the crystalline form. Background technique [0002] Carbapenem antibiotic drugs have a wide range of applications. Since the discovery of thiamycin in 1976, a series of new carbapenem antibiotics have been discovered and developed, such as imipenem, panipenem, meropenem, faropenem, biapenem and ritipenem etc. The most important feature of this kind of antibiotics is that they not only have strong antibacterial activity and broad antibacterial spectrum, but also are highly stable to various β-lactamases, and can still exert a strong antibacterial effect on cephalosporin-resistant bacteria. Bacteria do not have cross-resistance to this class of drugs and other β-lactam antibiotics. The development and application of carbapenem antibiotics is expected to become the first-line treatment drug for refractory severe infect...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D519/06A61K31/4192A61P31/04
Inventor 翁艳军王喜军袁淑杰赵玉新李国峰杨槐
Owner HARBIN PHARMA GRP CO LTD GENERAL PHARMA FACTORY
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