Method for synthesizing ceftriaxone sodium

A technology of ceftriaxone sodium and a compound, applied in the field of medicine, can solve problems such as affecting the production efficiency of manufacturers, and achieve the effects of avoiding amplification effect and simple steps

Inactive Publication Date: 2016-05-18
上海博速医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Although the current process can meet the basic needs of production, there is still considerable room for impro

Method used

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  • Method for synthesizing ceftriaxone sodium
  • Method for synthesizing ceftriaxone sodium
  • Method for synthesizing ceftriaxone sodium

Examples

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Example Embodiment

[0022] Example 1:

[0023] 15.9g of compound I (0.1mol, MW159) and 28.49g of compound II (0.11mol, MW259) were added to the reaction flask containing 3.18g of dimethyl carbonate, stirred at 30°C for 1 hour, and then 38.5g was added Compound III (0.11mol, MW350), add 3.18g PEG-800 while stirring, add 0.975g triethylamine after stirring for 10 minutes, stir and react at 8°C for 3 hours, then add 5w.t.% sodium hydroxide solution dropwise to pH=7, adding excess acetone to precipitate white crystals, and vacuum drying at 20°C to obtain 65.6 g of compound V (MW661). The yield is 99.2%, the purity is over 99.99%, and the total impurities are less than 0.01%.

Example Embodiment

[0024] Example 2:

[0025] 15.9g of compound I (0.1mol, MW159) and 31.08g of compound II (0.12mol, MW259) were added to a reaction flask containing 4.77g of dimethyl carbonate, stirred at 40°C for 2 hours, and then 42g of compound was added Ⅲ (0.12mol, MW350), add 4.77g PEG-800 while stirring, add 1.59g triethylamine after stirring for 20 minutes, stir at 10°C for 4 hours, then add 5w.t.% sodium hydroxide solution dropwise to pH =7, add excess acetone to precipitate white crystals, and vacuum-dried at 30°C to obtain 65.6 g of compound V (MW661). The yield is 99.2%, the purity is over 99.99%, and the total impurities are less than 0.01%.

Example Embodiment

[0026] Example 3:

[0027] 15.9g of compound I (0.1mol, MW159) and 28.49g of compound II (0.11mol, MW259) were added to the reaction flask containing 3.18g of dimethyl carbonate, stirred at 35°C for 1 hour, and then 38.5g was added Compound III (0.11mol, MW350), add 3.18g PEG-800 with stirring, add 0.975g triethylamine after stirring for 10 minutes, stir at 10°C for 4 hours, and then add 5w.t.% sodium hydroxide solution dropwise to pH=7, adding excess acetone to precipitate white crystals, and vacuum drying at 30°C to obtain 65.8 g of compound V (MW661). The yield is 99.5%, the purity is above 99.99%, and the total impurities are less than 0.01%.

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Abstract

The invention discloses a method for synthesizing ceftriaxone sodium. The method includes the steps that a compound I and a compound II are added into a reaction vessel containing dimethyl carbonate, a stirring reaction is carried out for 1-2 h at 30-40 DEG C, then a compound III is added, PEG-800 is added with stirring, triethylamine is added after stirring is carried out for 10-20 min, a stirring reaction is carried out for 3-4 h at 8-10 DEG C, then a sodium hydroxide solution is dripped till the pH is 7, excessive acetone is added, white crystals are separated out, and a compound V is obtained after drying. According to the method, 7-ACA, sulfo-triazine heterocycle and cefotaxime side chains are subjected to a one-pot reaction, and successive condensation is carried out without separation; no expensive agent is used in the reaction process, environment-friendly low-toxicity dimethyl carbonate is adopted as a reaction solvent, and in a homogeneous-phase environment formed by PEG-800, high-purity ceftriaxone sodium is obtained at a high yield through simple steps; in addition, the magnification effect is effectively avoided, and the method is particularly suitable for industrial production.

Description

technical field [0001] The invention relates to a synthesis method, in particular to a method for synthesizing ceftriaxone sodium in one pot. It belongs to the field of medical technology. Background technique [0002] Ceftriaxone Sodium (Rocephin) is a third-generation cephalosporin antibiotic with strong activity against Enterobacteriaceae. The MIC90 for Escherichia coli, Klebsiella pneumoniae, Enterobacter aerogenes, Citrobacter freundii, indole-positive Proteus, Pruvidenella and Serratia is between 0.12 and 0.25mg / Between L. Enterobacter cloacae, Acinetobacter and Pseudomonas aeruginosa were less sensitive to the drug. It has strong antibacterial effect on Haemophilus influenzae, Neisseria gonorrhoeae and Neisseria meningitidis, and also has good effect on hemolytic streptococcus and pneumococcus. The MIC for Staphylococcus aureus is 2-4mg / L. Methicillin-resistant staphylococci and enterococci were resistant to this drug. Most Bacteroides fragilis are resistant to...

Claims

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Application Information

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IPC IPC(8): C07D501/36C07D501/06
CPCC07D501/06C07D501/36
Inventor 蔡建萍
Owner 上海博速医药科技有限公司
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