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Sulbenicillin sodium and sulbenicillin sodium used for injection

A technology of sulfbenicillin sodium and triethylamine sulfophenylacetic acid, which is applied in the direction of active ingredients of heterocyclic compounds, freeze-dried transportation, antibacterial drugs, etc., and can solve problems such as poor operability, unstable product quality, and environmental pollution

Inactive Publication Date: 2011-08-24
辽宁科泰生物基因制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The existing synthesis method of sulbenicillin sodium has the problems of high impurity content, unstable product quality, poor operability, and environmental pollution caused by waste in the synthesis route

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] 1. Preparation of Sulbenicillin Silane.

[0039] Put 132Kg of dichloromethane, 20Kg of 6-APA and 42Kg of BSA into the reaction tank, stir until the solution is clear, continue to react for 1 hour, and cool to -5°C for use. Put 200Kg of dichloromethane and 29.4Kg of triethylamine sulfophenylacetic acid into the reaction tank, cool, put in 9.6Kg of triethylamine, cool down to -3°C, add 11.4Kg of pivaloyl chloride, control the temperature not to exceed 0°C, add After completion, the reaction was continued for 1 hour by keeping below 0°C. Combine the feed liquids, control the reaction temperature from -5°C to 5°C, and react for 1 hour. Concentrate the feed solution to dryness under reduced pressure in a water bath not exceeding 50°C, lower the temperature to below 30°C and put in 64Kg of acetone, concentrate to dryness under reduced pressure according to the above method, lower the temperature to below 30°C, put in 80Kg of acetone, stir and cool down to 0°C , keep the te...

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PUM

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Abstract

The invention provides a synthesis method of sulbenicillin sodium and sulbenicillin sodium used for injection, which comprises the concrete steps of: using 6-APA and BSA to synthesize an organic salt, and dissolving the organic salt into dichloromethane; using a sulphur phenylacetic acid triethylamine salt and pivaloyl chloride to make mixed anhydride; carrying out anhydrous condensation on the sulphur phenylacetic acid triethylamine salt and the pivaloyl chloride in the dichloromethane; and then forming a sodium salt, free-drying and obtaining a finished product. The new technical process is stable and feasible, better and stable in product quality and strong in operability of production, and reduces the environmental pollution.

Description

technical field [0001] The invention belongs to the field of medicine synthesis. Specifically, the present invention relates to a synthetic method of sulbenicillin sodium and sulbenicillin sodium for injection, and the sulbenicillin sodium and sulbenicillin sodium for injection obtained by said method. Background technique [0002] Sulbenicillin sodium is a broad-spectrum semi-synthetic penicillin antibiotic, which is effective against Enterobacteriaceae bacteria such as Escherichia coli, Proteus, Enterobacter, Citrobacter, Salmonella and Shigella, and Pseudomonas aeruginosa, Haemophilus influenzae, Neisseria and other Gram-negative bacteria have antibacterial effect. It also has antibacterial activity against hemolytic Streptococcus, Streptococcus pneumoniae and non-penicillinase-producing Staphylococcus. It also has a certain effect on anaerobic bacteria including Peptostreptococcus and Clostridium. The mechanism of action of sulbenicillin sodium is to play a bactericid...

Claims

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Application Information

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IPC IPC(8): C07D499/16C07D499/62A61K31/43A61K9/19A61P31/04
Inventor 陆夕明刘志隋巍峰陆文娟
Owner 辽宁科泰生物基因制药股份有限公司
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