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, uns

Method used

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Examples

Experimental program
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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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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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