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Process for dissolving 3,5-substituted oxazolidone

A compound, oxazolidinyl technology, applied in the field of dissolution of 3,5-substituted oxazolidinone compounds, can solve the problems of unstable performance, poor solubility, inability to be placed for a long time, etc., and achieve good stability Effect

Active Publication Date: 2009-04-01
广东金城金素制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical solution of the present invention is to provide a method for dissolving 3,5-substituted oxazolidinone compounds to solve the long-standing problems of poor solubility of such compounds, unstable performance after being formulated into test samples, and inability to obtain long-term placement problem

Method used

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  • Process for dissolving 3,5-substituted oxazolidone
  • Process for dissolving 3,5-substituted oxazolidone
  • Process for dissolving 3,5-substituted oxazolidone

Examples

Experimental program
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Effect test

Embodiment 1

[0122] In a 150ml beaker, accurately weigh (S)-[N-3-(3′-fluoro-4′-(4″-phenylpiperazinyl))phenyl-2-oxo-5-oxazolidine Base] methyl acetamide 0.2g, at room temperature 25 ℃, add glacial acetic acid 20ml, stir, shake well, after the solution is clarified, then add 10ml acetic anhydride, stir, shake well, after standing still to room temperature, can prepare The test solution for the determination of sample content by non-aqueous titration.

Embodiment 2

[0124] In a 50ml beaker, accurately weigh (S)-[N-3-(3′-fluoro-4′-(4″-phenylpiperazinyl))phenyl-2-oxo-5-oxazolidine Base] methyl acetamide 0.1g, at room temperature 25 ℃, add 0.2ml of formic acid to dissolve, stir, shake well, then add 10ml of methanol, stir, shake well, that is to prepare the test solution that can measure the sample content by high-efficiency liquid method .

[0125] Table 4 shows various conditions and dissolution rates of Examples 3 to 7 using part of the acidic solvent and Comparative Examples 1 to 4 using reagents other than the acidic reagent.

[0126] Table 4. Dissolution rates under various conditions

[0127] solvent temperature(℃) time (min) Dissolution rate (%) Example 3 hydrochloric acid 25 1 100 Example 4 phosphoric acid 25 2 100 Example 5 Malonate 25 2 100 Example 6 citric acid 25 2 100 Example 7

Embodiment 3

[0129] Accurately weighed (S)-[N-3-(3′-fluoro-4′-(4″-phenylpiperazinyl))phenyl-2-oxo-5-oxazolidinyl]methyl ethyl Amide 0.1g, add 2mol / L hydrochloric acid to dissolve, dilute with water to the required concentration and then prepare injection.

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Abstract

The present invention provides process of dissolving 3, 5-substituted oxazolidone. During its dissolving process, 3, 5-substituted oxazolidone is first dissolved in acid solvent completely and other solvent is then added to compound clarified solution. The process has high specificity, high dissolving speed, no need of special instrument and low cost, and is significant for the production and quality detection of 3, 5-substituted oxazolidone.

Description

technical field [0001] The invention provides a method for dissolving 3,5-substituted oxazolidinone compounds. The method is useful in the determination of the content of chemical raw materials and standardization of the content of reference substances and the injection of 3,5-substituted oxazolidinone compounds. The problem of solubility is solved in the liquid configuration to make it possible to operate. Background technique [0002] Antimicrobial resistance is a major problem facing the world today. Since the 1980s, multidrug-resistant Gram-positive bacteria have become the main pathogens of hospital-acquired pneumonia. At present, the treatment of Gram-positive bacterial infections is mostly caused by drug-resistant bacteria, so that there are very few therapeutic drugs available for clinical use, which has become a major clinical challenge. Staphylococci can acquire multidrug resistance, especially in nosocomial infections, but also in community-acquired infections. ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/496A61K31/5377A61K9/08A61K47/02A61K47/12
Inventor 王莹朱锦刘劲松鲁韬
Owner 广东金城金素制药有限公司