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Crystalline form III of oxazolidinone antibacterial drug free acid and preparation method and application of crystalline form III of oxazolidinone antibacterial drug free acid

A technology for antibacterial drugs and oxazolidinones, applied in the field of medicine, can solve the problem of high crystallinity, achieve good stability, significant economic and social benefits, and improve the effects of medicinal value and commercial value

Inactive Publication Date: 2019-08-16
碧豫药业有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The crystal form III of the free acid of an oxazolidinone antibacterial drug has high crystallinity and good stability in aqueous solution, and is suitable for preparing pharmaceutical preparations or pharmaceutical compositions, and is more suitable for preparing antibacterial drugs, but so far No public reports

Method used

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  • Crystalline form III of oxazolidinone antibacterial drug free acid and preparation method and application of crystalline form III of oxazolidinone antibacterial drug free acid
  • Crystalline form III of oxazolidinone antibacterial drug free acid and preparation method and application of crystalline form III of oxazolidinone antibacterial drug free acid
  • Crystalline form III of oxazolidinone antibacterial drug free acid and preparation method and application of crystalline form III of oxazolidinone antibacterial drug free acid

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Embodiment 1

[0020] In the specific implementation of the present invention, a method for preparing the crystal form III of the free acid of oxazolidinone antibacterial drugs is that the reaction process formula is:

[0021]

[0022] According to the above formula, a method for preparing the crystal form III of the free acid of an oxazolidinone antibacterial drug of the present invention comprises the following steps:

[0023] (1), add 100g of free acid precursor molecules to 4L of 1,4-dioxane to form a solution, then add the solution to 6M 30 equivalent hydrochloric acid solution at 0-5°C to form Reaction mixture; heat the reaction mixture to 55°C, stir at room temperature for 10 hours, then cool to 0-5°C, adjust the pH value to 2-3 with 1M 1 equivalent of NaOH, continue to stir at 0-5°C for 1 hour, filter , the filter cake was washed at 10-20° C. for 2 hours with 10 times the volume of methanol, filtered, and dried to obtain 89 g of oxazolidinone antibacterial drug free acids shown in...

Embodiment 2

[0026] A method for preparing crystal form III of oxazolidinone antibacterial drug free acid of the present invention, take 10g of the oxazolidinone antibacterial drug free acid free acid prepared in embodiment 1 step (1) without fixed solid, add water 200mL, Stir at 40°C for 60 hours, filter, and vacuum-dry the filter cake at 50°C for 28 hours to obtain 8.8 g of crystal form III solid with a yield of 88%. The obtained solid is subjected to powder X-ray diffraction, and its X-ray diffraction pattern is as follows: figure 1 shown.

[0027] The crystal form III prepared in Example 1 and Example 2 was determined by X-ray diffraction and contained the following characteristic peaks: 5.4±0.2°, 8.6±0.2°, 10.9±0.2°, 12.4±0.2°, 16.8± 0.2°, 20.0±0.2°, 21.1±0.2°, 21.9±0.2°, 22.3±0.2°, 22.6±0.2°, 24.1±0.2°, 24.9±0.2°, 26.2±0.2°, 27.4±0.2°, 29.8± 0.2°, this crystal form has high crystallinity and good stability in aqueous solution. It is suitable for the preparation of pharmaceutical pre...

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Abstract

The invention relates to a crystalline form III of an oxazolidinone antibacterial drug free acid and a preparation method and application of the crystalline form III of the oxazolidinone antibacterialdrug free acid. Preparation of the crystalline form III can be solved effectively, the crystallinity is changed, and the stability and medicinal value of the crystalline III in an aqueous solution are further increased. The preparation method comprises the steps: dissolving precursor molecules of the oxazolidinone antibacterial drug free acid in 1,4-dioxane so as to form a solution, then adding the solution to a hydrochloric acid solution at 0-5 DEG C, performing heating to 55 DEG C, performing stirring at room temperature for 10 hours, then performing cooling to 0-5 DEG C, adjusting the pH value with NaOH, keeping stirring, performing filtration, washing the filter cake with methanol, performing filtration and drying, adding the obtained amorphous solid of the oxazolidinone antibacterialdrug free acid in a solvent for dissolution, performing stirring at room temperature, performing filtration, and performing vacuum drying on the obtained filter cake so as to obtain the crystalline form III. The crystalline form III has good water solubility and excellent stability in an aqueous solution, is suitable for preparation of a pharmaceutical preparation or a pharmaceutical composition,and can be made into an antibacterial drug, and a new route is developed for antibacterial drugs.

Description

technical field [0001] The invention relates to medicine, in particular to a crystal form III of free acid of oxazolidinone antibacterial drugs and its preparation method and application. Background technique [0002] Due to the abuse of antibiotics in poultry feed and human diseases, the problem of bacterial resistance is becoming more and more serious. In the next few years, human beings will face the challenge of superbugs and lead to a situation where no drugs are available. As a result, countries have increased investment in the research and development of new antibacterial drugs, and have achieved gratifying results in recent years, including the crystal form B of an oxazolidinone antibacterial drug disclosed in Chinese patent CN106478723B and its preparation method And application, chemical structural formula is as shown in formula (1): [0003] [0004] Published data show that the compound represented by the formula (1) has stronger in vivo and in vitro antibact...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6561A61K31/675A61P31/04
CPCA61P31/04C07B2200/13C07F9/6561
Inventor 陈景才吴杰军
Owner 碧豫药业有限责任公司
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