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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

AI Technical Summary

Problems solved by technology

Although the current process can meet the basic needs of production, there is still considerable room for improvement in product yield and purity. These indicators directly affect the production efficiency of manufacturers.

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Add 15.9g of compound I (0.1mol, M.W.159) and 28.49g of compound II (0.11mol, M.W.259) into a reaction flask containing 3.18g of dimethyl carbonate, stir and react at 30°C for 1 hour, then add 38.5g Compound III (0.11mol, M.W.350), 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 dropwise 5w.t.% sodium hydroxide solution to When pH=7, excess acetone was added, white crystals were precipitated, and dried under vacuum at 20°C to obtain 65.6 g of compound V (M.W.661), with a yield of 99.2%, a purity of over 99.99%, and a total impurity of less than 0.01%.

Embodiment 2

[0025] Add 15.9g of compound I (0.1mol, M.W.159) and 31.08g of compound II (0.12mol, M.W.259) into a reaction flask containing 4.77g of dimethyl carbonate, stir and react at 40°C for 2 hours, then add 42g of compound Ⅲ (0.12mol, M.W.350), add 4.77g PEG-800 while stirring, add 1.59g triethylamine after stirring for 20 minutes, stir and react at 10°C for 4 hours, then add dropwise 5w.t.% sodium hydroxide solution to pH =7, adding excess acetone, white crystals were precipitated, and dried under vacuum at 30°C to obtain 65.6 g of compound V (M.W.661), with a yield of 99.2%, a purity of over 99.99%, and a total impurity of less than 0.01%.

Embodiment 3

[0027] Add 15.9g of compound I (0.1mol, M.W.159) and 28.49g of compound II (0.11mol, M.W.259) into a reaction flask containing 3.18g of dimethyl carbonate, stir and react at 35°C for 1 hour, then add 38.5g Compound III (0.11mol, M.W.350), add 3.18g PEG-800 while stirring, add 0.975g triethylamine after stirring for 10 minutes, stir and react at 10°C for 4 hours, then add dropwise 5w.t.% sodium hydroxide solution to When pH=7, excess acetone was added, and white crystals were precipitated, and vacuum-dried at 30°C to obtain 65.8 g of compound V (M.W.661), with a yield of 99.5%, a purity of over 99.99%, and a total impurity of 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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