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Synthesis method of azlocillin sodium

A technology of azlocillin sodium and a synthesis method, which is applied in the field of antibiotic drug synthesis, can solve the problems of unfavorable industrialized production, complicated process route and high cost, and achieves the effects of facilitating industrial production, simplifying the synthesis process and stable medicinal properties.

Inactive Publication Date: 2017-11-24
JIANGSU HI STONE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] The existing preparation method of azlocillin sodium has defects such as complex process route, low yield and high cost, which is unfavorable for industrialized production

Method used

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  • Synthesis method of azlocillin sodium

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Embodiment 1

[0029] (1) Dissolution of raw materials: Add 120ml of acetone, 200ml of purified water and 20g of ampicillin trihydrate to the reaction tank at 5°C. After stirring evenly, add triethylamine dropwise at a constant temperature until the solution is completely clarified to make ampicillin trihydrate. Water acid is completely dissolved;

[0030] (2) Condensation reaction: 1-chloroformyl-2-imidazolidine, which accounts for 1 / 2 of the mass of ampicillin trihydrate in step (1), was slowly added dropwise to the clear solution in step (1) at a rate of 5ml / min ketone, after stirring evenly, add triethylamine to adjust the pH value of the mixed solution to 7.5-10, and then react at a low temperature of 3-5 ℃ for 3.5 hours, so that the condensation reaction of ampicillin and 1-chloroformyl-2-imidazolidinone occurs, generate azlocillin acid solution;

[0031] (3) Purification treatment: stop stirring, add medicinal activated carbon accounting for 0.3% of the mass of the reaction solution ...

Embodiment 2

[0038] A kind of synthetic method of azlocillin sodium, comprises the steps:

[0039] (1) Dissolution of raw materials: Add 150ml of acetone, 240ml of purified water and 25g of ampicillin trihydrate into the reaction tank at 12°C. Acid is completely dissolved;

[0040] (2) Condensation reaction: Slowly add 1-chloroformyl-2-imidazolidine which accounts for 1 / 2 of the mass of ampicillin trihydrate in step (1) to the clear solution in step (1) at a rate of 8ml / min Ketone, after stirring evenly, add triethylamine to adjust the pH value of the mixed solution to 7.5-10, and then react at a low temperature of 5°C for 3.5 hours to make ampicillin and 1-chloroformyl-2-imidazolidinone undergo condensation reaction to form albino Loxillin acid solution;

[0041] (3) Purification treatment: stop stirring, add medicinal activated carbon accounting for 0.35% of the mass of the reaction liquid to the reaction liquid obtained in step (2), cover the feeding port, start stirring, decolorize f...

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Abstract

The invention discloses a synthesis method of azlocillin sodium. The synthesis method comprises the following steps: (1) dissolving raw materials; (2) carrying out condensation reaction; (3) carrying out purification treatment; (4) preparing finished-product azlocillin; (5) carrying out salt formation reaction; (6) filtering and degerming; (7) freezing and drying. According to the synthesis method of the azlocillin sodium, disclosed by the invention, a synthesis process is simplified effectively and reaction conditions are moderate; the feasibility of implementation is high and the raw materials are easily obtained; the controllability of a synthesis technology is relatively good and industrial production is convenient to realize; the obtained azlocillin sodium has the advantages of high yield, great purity and stable drug property and has a wide market prospect.

Description

technical field [0001] The invention relates to the technical field of antibiotic drug synthesis, in particular to a method for synthesizing azlocillin sodium. Background technique [0002] Azlocillin sodium (Azlocillin sodium), also known as benzimidazole penicillin, chemical name is (2S,5R,6R)-3,3-dimethyl-6-[(R)-2-(2-oxo-1 - Imidazolidinecarboxamido-2-phenylacetamido)-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate, sodium salt. [0003] [0004] Molecular formula: C20H22N5NaO6S [0005] Molecular weight: 483.47 [0006] It is a semi-synthetic urea penicillin, pioneered by the United Kingdom, and has been clinically applied in Germany, the United Kingdom, the United States and Japan. my country issued a new drug certificate and a production license to Zhejiang Kangenbei Group Co., Ltd. in January 1996, and the company produced Alexin injection powder. [0007] The existing preparation method of azlocillin sodium has the defects of complicated process route, l...

Claims

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Application Information

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IPC IPC(8): C07D499/68C07D499/16C07D499/18
CPCC07D499/68C07D499/16C07D499/18
Inventor 王多平卫耿虎史加桂夏晓霞
Owner JIANGSU HI STONE PHARMA
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