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Synthesis of austrastaph

A technology of o-benzyl penicillin and synthesis process, applied in directions such as organic chemistry, can solve problems such as difficult process, difficult to obtain solid powder, etc., and achieve the effects of simple process, easy industrial production, and easy operation

Active Publication Date: 2005-05-11
石药集团中诺药业(石家庄)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because of the viscosity of cloxacillin acid, it is not easy to make solid powder, which will cause certain difficulties to the process

Method used

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  • Synthesis of austrastaph
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Examples

Experimental program
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Effect test

Embodiment 1

[0020] Measure 250L of 95% alcohol and 50L of deionized water, add them to the condensation tank in turn, prepare the aqueous solution of alcohol, start stirring and jacket cooling water, and then add 20kg of 6-APA. Insert the electrodes of the thermometer and the pH meter into the feed solution. When the temperature drops below 15°C, start to add a 10% NaOH solution into the tank to keep the pH value at 7-8 until the 6-APA gradually dissolves.

[0021] According to the molar ratio of 6-APA and o-chlorobenzisoxazole chloride as 1: (0.95-1.15), weigh o-chlorobenzisoxazole chloride, when the temperature of the 6-APA solution is cooled to below 10°C , began to add o-chlorobenzisoxazole chloride to the tank. Then start to add 10% NaOH solution, control the pH value in the tank to 6-7, and the temperature does not exceed 20° C. until the pH value is stable at 6.5 and the reaction solution is clear.

[0022] Add air pressure to the condensation tank, and press it into the crystalli...

Embodiment 2

[0028] Measure 50L of acetone and 50L of deionized water, add them to the condensation tank in turn to prepare an aqueous solution of acetone; turn on the stirring and jacket cooling water, and then add 20kg of 6-APA. Insert the electrodes of the thermometer and the pH meter into the feed solution. When the temperature drops below 15°C, start to add a 10% NaOH solution into the tank to keep the pH value at 7-8 until the 6-APA gradually dissolves.

[0029] According to the molar ratio of 6-APA and o-chlorobenzisoxazole chloride as 1: (0.95-1.15), weigh o-chlorobenzisoxazole chloride, when the temperature of the 6-APA solution is cooled to below 10°C , began to add o-chlorobenzisoxazole chloride to the tank. Then start to add 10% NaOH solution, control the pH value in the tank to 6-7, and the temperature does not exceed 20° C. until the pH value is stable at 6.5 and the reaction solution is clear.

[0030] Add air pressure to the condensation tank, and press it into the crystal...

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Abstract

Synthesis of cloxacillin benxethine is carried out by: dissolving 6-aminopenicillanic acid in aqueous organic solvent to form a sodium salt, condensing with o-chlorbenzylisoxazoleacyl cyanide to obtain cloxacillin benxethine solution directly, and having metathesis with N,N-dibenzyl quadol diacetate. It is simple and costs low.

Description

technical field [0001] The invention relates to a synthesis process of o-chlorobenzathine penicillin. technical background [0002] O-chlorobenzathine penicillin is a semi-synthetic penicillin for veterinary use, mainly used to treat cow mastitis, bovine cornea, conjunctivitis, etc. Spanish patent ES447058 discloses a kind of synthetic technique of cloxacillin penicillin, is that cloxacillin acid is dissolved in dilute lye, obtains cloxacillin sodium salt, and then with N,N-dibenzylethylenediamine diacetic acid ( Abbreviated as DBED) by metathesis reaction. Because cloxacillin acid is viscous, it is difficult to obtain solid powder, which will cause certain difficulties to the process. Contents of the invention [0003] The technical problem to be solved by the present invention is to provide a synthesis process of o-chlorobenzathine penicillin with simple process, convenient operation, low cost and easy industrial production. ...

Claims

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Application Information

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IPC IPC(8): C07D499/76
Inventor 李勇张延峰张勇张立辉吴爱宝郭惠娟
Owner 石药集团中诺药业(石家庄)有限公司
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