Method for preparing cefepime dihydrochloride

A technology of cefepime hydrochloride and cephalosporin, applied in the field of preparation of cefepime hydrochloride, can solve the problems of insufficient supply, high price, inconvenient post-processing, etc.

Inactive Publication Date: 2015-08-05
CHANGCHUN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The reaction conditions of this route are mild, but the problem is that firstly, there are a large number of isomers in the final product, which needs to go through a chromatographic purification step, and the post-treatment of the process is more complicated.
This reaction route uses ethyl acetate instead of carbon tetrachloride as the reaction solvent, but it still inevitably produces a large number of isomerized products, which requires a complicated separation process and is not convenient for post-processing. In addition, the domestic supply of the reaction raw material ACLH is insufficient. , expensive and therefore unsuitable for industrial production

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  • Method for preparing cefepime dihydrochloride

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Embodiment 1

[0015] Example 1 A preparation method of cefepime hydrochloride. The steps and conditions are as follows:

[0016] The invention provides a preparation method of cefepime hydrochloride. The steps and conditions are as follows:

[0017] (1) The raw materials are: 7-Aminocephalosporanic acid (abbreviated as 7-ACA), hexamethyldisilazane (abbreviated as HMDS), trimethyliodosilane (abbreviated as TMSI), N-methylpyrrolidine (abbreviated as NMP); CH 3 OH (methanol); the mass ratio of raw material components is 7-ACA: HMDS: catalyst: TMSI: NMP: CH 3 OH=1:3:0.02:1.8:3:1; the catalyst is 95% hydrochloric acid;

[0018] (2) The crude product of cefepime hydrochloride was prepared as follows: According to the mass ratio of raw materials, under the protection of dry nitrogen, add 5.0g of 7-ACA to a dry 100mL three-necked flask, press CH 3 OH mass g: the volume of anhydrous dichloromethane mL is 1: 50 Add anhydrous dichloromethane, stir, heat at 45°C for 3 h, add 15 g of HMDS, add ...

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Abstract

The invention provides a method for preparing cefepime dihydrochloride. The method employs the raw materials of 7-ACA, HMDS, TMSI, NMP and CH3OH, and a catalyst is hydrochloric acid having 98% of concentration. According to the invention, the method employs a one kettle way, a cefepime dihydrochloride crude product is prepared, then the cefepime dihydrochloride crude product is purified, and finally cefepime dihydrochloride is obtained. The purity of the cefepime dihydrochloride is 97%, yield can reach 31.3%, compared with the current synthesis technology, the yield is increased by 3.3-10% (by metering with 7-ACA), and the purity is increased by 4%. The preparation method has the advantages that the industrial production requirements of short reaction period, easily available raw materials and low cost can be satisfied, and has industrial application.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to a preparation method of cefepime hydrochloride. Background technique [0002] Cefepime dihydrochloride, whose trade name is Maxipime, was developed by Bristol-Myers Squibb Pharmaceutical Ltd. and launched in Sweden in 1993. As the fourth-generation cephalosporin for injection, cefepime has broad-spectrum antibacterial activity against Gram-positive bacteria, negative bacteria and anaerobic bacteria, and has enhanced resistance to Gram-positive bacteria compared with the previous third-generation varieties. The activity of Streptococcus and Streptococcus pneumoniae is greatly enhanced. It is currently used clinically to prevent and treat a variety of bacterial infectious diseases. It is a widely used antibiotic product. [0003] The synthesis of cefepime hydrochloride mainly contains the following several methods at present: [0004] 1) Using 7-phenylacetamide amino-3-chloromethy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/46C07D501/04C07D501/12
CPCC07D501/46C07D501/04C07D501/12
Inventor 张龙崔庆雨
Owner CHANGCHUN UNIV OF TECH
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