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Method for preparing cefepime hydrochloride

A technology of cefepime hydrochloride and hydrochloric acid, which is applied in the preparation field of cefepime hydrochloride, can solve the problems of poor fluidity of cefepime hydrochloride, harsh reaction conditions, uneven crystal form and the like, and achieves good fluidity, fast reaction speed, The effect of low production cost

Inactive Publication Date: 2012-09-19
苏州盛达药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The cefepime hydrochloride prepared by the prior art generally has the defects of poor fluidity, high impurity content and inhomogeneous crystal form, while the traditional preparation method has defects such as harsh reaction conditions, complicated process, low yield, and low product purity. Therefore it is necessary to study a new preparation method of cefepime hydrochloride with simple process, uniform product crystal form and good fluidity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] (1) Add 20g of 7-ACA dissolved in 140ml of anhydrous cyclohexane into a clean and dry flask, stir at room temperature for 5min, add 18.6ml of hexamethyldisilamine and 0.4ml of iodotrimethylsilane, the whole reaction system Vacuum reflux at 55°C for 12 hours, cool down to 10°C and add 40ml of anhydrous cyclohexane to dilute, cool down to 5°C, add 10.68ml of N-methylpyrrolidone dropwise under nitrogen protection, and control the temperature of the entire reaction system to less than 5°C Add 18.8ml iodotrimethylsilane and 0.5g imidazole, stir for 30min, gradually raise the temperature of the whole reaction system to 40°C, continue stirring for 23h until the mass content of 7-ACA in the whole reaction system is less than 2%;

[0019] (2) Add 40ml of cyclohexane and 10ml of methanol, keep the temperature of the entire reaction system at 0-5°C, stir for 15min, filter, wash with 1×40ml of cyclohexane, methanol / water, acetone, and dry to obtain 28g of crude product;

[0020] (3...

Embodiment 2

[0023] (1) Add 20g of 7-ACA dissolved in 140ml of anhydrous cyclohexane into a clean and dry flask, stir at room temperature for 5min, add 18.6ml of hexamethyldisilamine and 0.4ml of iodotrimethylsilane, the whole reaction system Vacuum reflux at 55°C for 12 hours, cool down to 10°C and add 40ml of anhydrous cyclohexane to dilute, cool down to 5°C, add 10.68ml of N-methylpyrrolidone dropwise under nitrogen protection, and control the temperature of the entire reaction system to less than 5°C Add 18.8ml iodotrimethylsilane and 0.5g imidazole, stir for 30min, gradually raise the temperature of the whole reaction system to 40°C and continue stirring for 23h until the mass content of 7-ACA in the whole reaction system is less than 2%;

[0024] (2) Add 100ml of anhydrous cyclohexane and 10ml of methanol, keep the temperature of the whole reaction system at 5°C, then add 50ml of 3mol / L HCl, heat the whole reaction system to 20-25°C for hydrolysis, keep the temperature of the whole re...

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PUM

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Abstract

The invention discloses a method for preparing cefepime hydrochloride. The method comprises the following steps of: adding hexamethyldisilazane and trimethylsilyl iodide into 7-aminocephalosporanic acid (ACA), performing vacuum reflux at the temperature of 55 DEG C for 12h, reducing the temperature, diluting, adding N-methylpyrrolidone and trimethylsilyl iodide, reacting at the temperature of 40 DEG C for 23h, after-treating and recrystallizing to obtain 7-ACMP.HCl, dissolving the 7-ACMP.HCl into a solvent at the temperature of 0 to 5 DEG C, adding a small amount of AE-active ester and triethylamine for multiple times, and treating to obtain the cefepime hydrochloride after the reaction is finished. The method for preparing the cefepime hydrochloride is high in reaction speed, low in production cost, and high in product purity and flowability.

Description

technical field [0001] The invention relates to the field of chemical pharmacy, in particular to a preparation method of cefepime hydrochloride. Background technique [0002] Cefepime hydrochloride, chemical name: (6R,7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-methoxyimine]acetamido-3-[1 -(1-Methylpyrrolidinyl)methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate hydrochloride monohydrate. Cefepime hydrochloride is a fourth-generation cephalosporin with broad-spectrum and high-efficiency characteristics. It achieves bactericidal effect by inhibiting the biosynthesis of bacterial cell walls. Compared with third-generation cephalosporins, it has a stronger effect on Gram-positive bacteria activity, and has higher stability and lower inducibility to the lactamase produced by bacteria, and has a wider antibacterial spectrum. [0003] The cefepime hydrochloride prepared by the prior art generally has the defects of poor fluidity, high impurity content and inhomogeneous crys...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/46
Inventor 曾润保王芳黄建忠何静
Owner 苏州盛达药业有限公司
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