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Synthesis method of cefotaxime sodium

A technology of cefotaxime sodium and a synthetic method, applied in the direction of organic chemistry, etc., can solve problems such as industrial production safety hazards, affecting product purity, affecting production environment, etc., achieving high safety, low production energy consumption, and high reaction yield Effect

Active Publication Date: 2016-06-08
HARBIN HEJIA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The two-step process has problems such as low product yield, poor quality, large amount of solvent used, serious pollution, and large power consumption.
At present, the research on the preparation of cefotaxime sodium by one-step synthesis method has been reported. For example, Chinese patent ZL200510118235.1 discloses a preparation process of cefotaxime sodium. Under the action of reaction, add benzothiazole cosolvent, then add sodium salt forming agent to carry out reaction and precipitate crystallization and make, this method adopts one-step process operation, has improved product yield, has reduced production cost, but preparation process 7- The reaction of ACA and AE-active ester still needs to be carried out under the effect of amine intermediate reactant, also needs to use benzene type organic solvent or other organic solvents as auxiliary solvent, and the use of amine intermediate reactant and auxiliary solvent causes in the product Solvent residues affect the purity of the product, and also affect the production environment, bringing safety hazards to industrial production

Method used

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Embodiment 1

[0024] This embodiment relates to the synthesis of a group of cefotaxime sodium.

Embodiment 11

[0026] Present embodiment relates to the synthesis of cefotaxime sodium, and this synthetic method comprises the following steps:

[0027] a. Synthesis reaction: Add 500L of acetone and 60L of water in turn into the condensation reaction tank, start stirring and cool down to 10°C, add 70kg of 7‐ACA, 95kg of AE active ester, stir for 10 minutes, then cool down to 10°C, Slowly add 12% (mass fraction) sodium hydroxide solution dropwise while stirring within 1 minute, and stir the solution until it becomes clear, and make the solution pH reach 9.5 by detecting the pH value of the solution, stop dropping, start timing, and continue stirring at 15°C React for 60 to 90 minutes. After the reaction reaches 60 minutes, start sampling and measure the residual 7-ACA content in the solution by high-performance liquid chromatography (HPLC). When the residual 7-ACA content is less than or equal to 0.5%, stop stirring and react to obtain a reaction solution;

[0028] B, decolorization, filtra...

Embodiment 12

[0035] Present embodiment relates to the synthesis of cefotaxime sodium, and this synthetic method comprises the following steps:

[0036]a. Synthesis reaction: Add 500L of acetone and 70L of water in turn into the condensation reaction tank, start stirring and cool down to 5°C, add 70kg of 7‐ACA, 98kg of AE active ester, stir for 15 minutes, then cool down to 5°C, Slowly add 11% (mass fraction) sodium hydroxide solution dropwise while stirring within 1 minute, and stir the solution until it becomes clear, and make the solution pH reach 9.3 by detecting the pH value of the solution, stop dropping, start timing, and continue stirring at 20°C React for 60 to 90 minutes. After the reaction reaches 60 minutes, start sampling and measure the residual 7-ACA content in the solution by high-performance liquid chromatography (HPLC). When the residual 7-ACA content is less than or equal to 0.5%, stop stirring and react to obtain a reaction solution;

[0037] B, decolouring, filtration: ...

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Abstract

The invention relates to a synthesis method of cefotaxime sodium. The method includes the steps that with an acetone-water solution as a solvent, 7-ACA and AE-active ester are subjected to a stirring reaction for 5-15 min; then, a sodium hydroxide solution is added with stirring for a reaction, obtained reaction liquor is filtered and then crystallized with acetone, and the product cefotaxime sodium is obtained. By the adoption of the one-step synthesis method, the reaction yield is high, product quality is stable, and the operation process is simple and convenient; moreover, no amine intermediate reactant or cosolvent is used, so that production safety is high.

Description

technical field [0001] The invention relates to the technical field of compound preparation, in particular to a synthesis method of cefotaxime sodium. Background technique [0002] Cefotaxime sodium (cefotaximesodium) belongs to the third-generation cephalosporin derivatives, has the advantages of broad antibacterial spectrum, strong antibacterial effect, and small toxic and side effects. It is clinically used in the treatment of various sensitive bacterial infections. Its molecular formula is C 16 h 16 N 5 o 7 S 2 Na, the molecular weight is 477.44, the chemical name is (6R,7R‐3‐[(acetoxy)methyl]‐7‐[(2‐amino‐4‐thiazolyl)‐(methoxyimino)acetamide ]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-formic acid sodium salt. The traditional preparation process of cefotaxime sodium is a two-step synthesis method, that is, the first 7‐ACA (also known as 7‐aminocephalosporanic acid) and AE‐active esters (also known as 2‐(2‐amino‐4‐thiazolyl)‐2‐(methoxyoxo Amino) thiobenzothiazolyl ...

Claims

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Application Information

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IPC IPC(8): C07D501/34C07D501/04C07D501/12
CPCC07D501/04C07D501/12C07D501/34
Inventor 刘振强金石马宝利张磊李宝云
Owner HARBIN HEJIA PHARMA CO LTD
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