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Synthesis process of o-chloro-benzathine penicillin

A technology of o-benzyl penicillin and synthesis process, applied in directions such as organic chemistry, can solve the problems of complex production process, difficult implementation of technical process, low production efficiency, etc., achieves overcoming many processes, improves single-pass conversion rate and product productivity, improve work efficiency

Inactive Publication Date: 2016-05-11
QINGDAO SHOUTAI AGRI SCI & TECH CO LTD
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AI Technical Summary

Problems solved by technology

In the current preparation process method of o-clobenzine penicillin, the technical process is not easy to implement, the purity of the o-clobenzine penicillin generated is low, the single-pass conversion rate of reactants is low, the production process is complicated and pollutes the environment relatively large, the production efficiency is low and high cost

Method used

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Embodiment

[0015] The o-chlorobenzathine penicillin synthesis technique of the present embodiment comprises the following steps:

[0016] (1) According to the ratio of organic solvent to water (1-3): 1, prepare an aqueous solution of organic solvent, add it to the condensation tank, turn on the stirring and jacket cooling water, and use 99-210 grams per liter of organic solvent Add 6-aminopenicillanic acid into the aqueous solution; when the temperature drops below 16°C, start to add 12% NaOH solution into the tank to keep the pH value at 8-9 to gradually dissolve 6-aminopenicillanic acid until;

[0017] (2) The molar ratio of 6-aminopenicillanic acid and o-chlorobenzisoxazole chloride is 1: (0.95-1.15) to weigh o-chlorobenzisoxazole chloride, when the above (1) step When the temperature of the sodium salt solution in the solution is cooled to below 10°C, start to add the weighed o-chlorobenzisoxazole chloride into the tank, then start to add the NaOH solution with a concentration of 13...

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Abstract

The invention discloses a synthesis process of o-chloro-benzathine penicillin. 6-aminopenicillanic acid is firstly dissolved in a dilute alkali solution to be prepared into sodium salt in an aqueous solution of an organic solvent, then subjected to condensation with isoxazolyl o-chlorobenzoyl chloride to directly obtain a cloxacillin sodium solution, and the cloxacillin sodium solution is subjected to double decomposition reaction with N, N-dibenzyl ethylenediamine diacetate to obtain the o-chloro-benzathine penicillin. The synthesis process of the o-chloro-benzathine penicillin disclosed by the invention has benefits of simple process, simple and convenient operation, low cost and easy industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and in particular relates to a synthesis process of o-chlorobenzathine penicillin. Background technique [0002] The synthesis process of o-chlorobenzathine penicillin at least includes basic processes such as esterification reaction, salt formation reaction and stirring. In the current preparation process method of o-clobenzine penicillin, the technical process is not easy to implement, the purity of the o-clobenzine penicillin generated is low, the single-pass conversion rate of reactants is low, the production process is complicated and pollutes the environment relatively large, the production efficiency is low and The cost is high. Contents of the invention [0003] In order to overcome the above-mentioned technical problems existing in the prior art field, the object of the present invention is to provide a synthetic process for o-clobenzine penicillin. The present inventi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/76C07D499/12C07D499/20
Inventor 张晶
Owner QINGDAO SHOUTAI AGRI SCI & TECH CO LTD
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