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Method for preparing azlocillin sodium

A technology of azlocillin sodium and azlocillin acid, applied in the direction of organic chemistry, etc., can solve the problems of complex reaction, large usage, complicated process, etc.

Inactive Publication Date: 2012-03-07
海南美好西林生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In the process of esterification and condensation, the use of organic matter is large, the reaction is complicated, the process is complicated, the purity of the obtained azlocillin sodium is low, and the production cost is correspondingly increased.
In response to this situation, we provide a simple synthesis method, through a one-step salt-forming reaction, which reduces the shortcomings of the cumbersome reaction process, so as to ensure the azlocillin sodium with high purity and stable quality

Method used

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  • Method for preparing azlocillin sodium

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Effect test

Embodiment 1

[0016] According to the preparation method of the azlocillin sodium of the present embodiment, it comprises the following steps successively:

[0017] (1) Prepare 5% sodium hydroxide solution for later use; weigh a certain amount of azlocillin acid and dissolve it in water to make a 40% aqueous solution of azlocillin sodium, place it in a low-temperature tank to cool, stir to cool down to 10°C, add Sodium salt-forming agent solution, stir until the solution is completely clear, filter, sterilize, and set aside;

[0018] (2) Place the above filtrate in a freeze-drying tray with a liquid layer thickness of 10-15mm, put it in the cold trap of a freeze dryer, pre-freeze-dry it at -35°C for 2 hours, and then vacuum freeze-dry it. The first stage:- 40℃~-5℃, the time is 5.5 hours; the second stage: -5℃~0℃, the time is 3.5 hours; the third stage: 0℃~30℃, the time is 1 hour, 30℃ continue to keep warm for about 4 hours, After the freeze-drying is finished, loose white azlocillin sodium...

Embodiment 2

[0020] According to the preparation method of the azlocillin sodium of the present embodiment, it comprises the following steps successively:

[0021] (1) Prepare 10% sodium isooctanoate and sodium carbonate mixed solution for subsequent use; take a certain amount of azlocillin acid and dissolve it in water to make a 60% aqueous solution of azlocillin sodium, place it in a low-temperature tank for cooling, and stir to cool down to 10°C, add sodium salt-forming agent solution, stir until the solution is completely clear, filter, sterilize, and set aside;

[0022] (2) Place the above filtrate in a freeze-drying tray with a liquid layer thickness of 10-15mm, put it in the cold trap of a freeze dryer, pre-freeze-dry it at -35°C for 2 hours, and then vacuum freeze-dry it. The first stage:- 40℃~-5℃, the time is 5.5 hours; the second stage: -5℃~0℃, the time is 3.5 hours; the third stage: 0℃~30℃, the time is 1 hour, 30℃ continue to keep warm for about 4 hours, After the freeze-drying...

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Abstract

The invention relates to a method for preparing azlocillin sodium. An azlocillin acid is subjected to once salt-forming reaction and then is freeze-dried, thereby acquiring freeze-dried powder of the azlocillin sodium. The method has the advantages of convenient operation, low cost and short production cycle. The acquired freeze-dried powder of the azlocillin sodium is stable in quality, high in purity and excellent in water-solubility.

Description

technical field [0001] The invention relates to the field of drug synthesis, and more particularly to a preparation method of azlocillin sodium used for antibacterial treatment. Background technique [0002] Azlocillin sodium English name: AzlocillinSodium, chemical name: (2S, 5R, 6R)-3.3-dimethyl-6-[(R)-2-(2-oxo-1-imidazolidinecarboxamide) -2-Phenylacetamido]-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid sodium salt. The chemical structure is as follows: [0003] [0004] This product is a penicillin antibiotic, which belongs to the third-generation broad-spectrum semi-synthetic penicillin. It is effective against G+ bacteria, G- bacteria and anaerobic bacteria, and can strongly resist Pseudomonas aeruginosa. It is suitable for G+ bacteria, G- bacteria and anaerobic bacteria. caused infection. The traditional synthetic route reported at present has two kinds that take 6-APA as raw material and ampicillin as raw material, and azlocillin sodium is obtained a...

Claims

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Application Information

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IPC IPC(8): C07D499/68C07D499/16
Inventor 魏雪纹李强梁勇魏西雨
Owner 海南美好西林生物制药有限公司
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