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Preparation method of oxacillin sodium and oxacillin sodium for injection

A technology for synthesizing oxacillin sodium and oxacillin is applied in the preparation of oxacillin sodium and oxacillin sodium for injection, and in the field of oxacillin sodium and oxacillin sodium for injection products, and achieves high stability The effect of stability, high purity and stability, and stable operation

Active Publication Date: 2011-08-24
山东二叶制药有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Also do not propose a kind of oxacillin sodium synthetic method that is suitable for industrial scale at present in this area

Method used

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  • Preparation method of oxacillin sodium and oxacillin sodium for injection
  • Preparation method of oxacillin sodium and oxacillin sodium for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1 Synthesis of Oxacillin Sodium.

[0047] condensation

[0048] Add 4200L of purified water to the condensation tank, control the temperature to 26°C~27°C, and put in 17.5kg Na 2 HPO 4 and 1.65kg NH 4 Cl was dissolved, and 93kg of 6-APA and 100kg of acid chloride were added. Add 6mol / L NaOH solution to adjust the pH to 6.5~7.0, and react for 2 hours. Control the reaction process temperature at 25°C~28°C, pH6.5~7.0. After the reaction is over, add 3 kg of medicinal activated carbon, and filter the clarified solution after 5 to 10 minutes and add it to the primary acidification tank.

[0049] acidified extraction

[0050] Primary acidification: Add 1100~1200L butyl acetate to the primary acidification tank, add all the condensation filtrate, control the temperature at 10~12°C, and start adding 6mol / LH 2 SO 4 , adjust the pH to 1.8~2.0, and after standing for 30 minutes, add the lower aqueous phase into the secondary acidification tank.

[0051] Seco...

Embodiment 2

[0060] Example 2 Synthesis of Oxacillin Sodium.

[0061] condensation

[0062] Add 4200L of purified water to the condensation tank, control the temperature to 27°C~28°C, and put in 17.5kg Na 2 HPO 4 and 1.65kg NH 4 Cl was dissolved, and 93kg of 6-APA and 100kg of acid chloride were added. Add 6mol / L NaOH solution to adjust the pH to 6.5~7.0, and react for 2 hours. Control the reaction process temperature at 28°C~30°C, pH6.5~7.0. After the reaction is over, add 3 kg of medicinal activated carbon, and filter the clarified solution after 5 to 10 minutes and add it to the primary acidification tank.

[0063] acidified extraction

[0064] Primary acidification: Add 1100~1200L butyl acetate to the primary acidification tank, add all the condensation filtrate, control the temperature at 12~15°C, and start adding 6mol / LH 2 SO 4 , adjust the pH to 1.8~2.0, and after standing for 30 minutes, add the lower aqueous phase into the secondary acidification tank.

[0065] Seco...

Embodiment 3

[0074] Embodiment 3 Detection of product quality.

[0075] Utilize the routine detection method that detects semi-synthetic penicillins, the products of each 3 batches that embodiment 1 and embodiment 2 make are detected, and average yield reaches 93.0%, and quality detection result is as follows:

[0076]

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Abstract

The invention provides a method for preparing oxacillin sodium and oxacillin sodium for injection by taking 6-APA and benzyl chloride isoxazole as raw materials, which comprises the steps of condensation, acidification, crystallization, crystal washing, grinding, packaging and the like. The synthesis method of the oxacillin sodium can be stably operated with high efficiency on a large scale, and realizes the synthesis of the oxacillin sodium with high yield, purity and stability on the industrial scale; and furthermore, the method can be used for directly obtaining the oxacillin sodium product for injection by controlling the production environment and process.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and specifically, provides a preparation method of oxacillin sodium and oxacillin sodium for injection, and also provides oxacillin sodium and oxacillin sodium for injection products prepared by the method . Background technique [0002] Oxacillin sodium is a semi-synthetic penicillin synthesized from 6-APA (6-aminopenicillanic acid), which has the characteristics of acid resistance and enzyme resistance, and is used for various infections caused by penicillin-resistant Staphylococcus, such as sepsis, respiratory tract Infection, meningitis, soft tissue infection, etc., as well as mixed infections caused by Streptococcus pyogenes or pneumococcus and penicillin-resistant Staphylococcus, are clinically effective first-line drugs with less toxic and side effects and low price. It was designated as a national drug in 1998. Essential medicines, recorded in the 24th edition of the United States Pharmacop...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/16C07D499/76A61K31/431A61K9/19A61P31/04
Inventor 朱炜陈学文陆夕明顾丰
Owner 山东二叶制药有限公司
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