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Method for preparing cefotetan bisodium

A technology of cefotetan disodium and cefene, which is applied in the field of preparation of beta-lactam antibiotic cefotetan disodium, can solve the problems of being unfavorable to large-scale industrialized production, high production cost, long route and the like

Inactive Publication Date: 2007-10-10
上海医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method route is longer, and production cost is higher, is unfavorable for large-scale industrialized production

Method used

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  • Method for preparing cefotetan bisodium
  • Method for preparing cefotetan bisodium
  • Method for preparing cefotetan bisodium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0018] 1 Preparation of 7-β-bromoacetamide-7α-methoxyl group-3-(1-methyl-1H-5-tetrazolyl)thiomethyl-3-cephem-4-carboxylic acid benzhydryl ester ( III)

[0019]

[0020] ethyl acetate

140L

7-MAC

3.36kg

7mol

N,N-Dimethylaniline

840g

7mol

bromoacetyl bromide

1.4kg

7mol

0.1N hydrochloric acid

35L

Anhydrous Magnesium Sulfate

Appropriate amount

[0021] Add 70L ethyl acetate, 7β-amino-7α-methoxy-3-(1-methyl-1H-5-tetrazolyl)thiomethyl-3-cephem-4-carboxylic acid di Benzyl ester (3.3kg, 7mol), stir to dissolve, cool in ice water to 0°C, add (840g, 7mol) N,N-dimethylaniline, add dropwise (1.4kg, 7mol) bromine under ice cooling Acetyl bromide, continue stirring at this temperature for 10 min, and add 35L of ice water and 70L of ethyl acetate to the reaction solution. The organic layer was washed three times with 12L of 0.1N hydrochloric acid solution, and dried over anhydrous mag...

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Abstract

This invention provides a method for preparing disodium cefotetan. The method has such advantages as abundant raw material (7-BAMCA), mild reaction conditions, no need for separation and purification of intermediate, and easy operation, thus is suitable for industrialization.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry. It specifically relates to a preparation method of cefotetan disodium, a β-lactam antibiotic. Background technique [0002] Infectious disease is the most common clinical disease, involving almost all clinical specialties, and it is also one of the most common causes of patient death. According to the report of the World Health Organization in 1997, the number of deaths from infectious diseases was as high as 33.3% of the total number of deaths from various causes. In China, the main diseases that endanger people's health are still infectious diseases caused by various pathogenic bacteria, and they are also the main cause of disability and death. [0003] Anti-infective drugs are a powerful weapon for human beings to fight against infectious diseases. They are the largest in number, most in variety, and fastest growing, and the market demand for drugs in this area has always been ve...

Claims

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Application Information

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IPC IPC(8): C07D501/04C07D501/36
Inventor 初秀梅刘辉崔万胜傅自勤
Owner 上海医药科技发展有限公司
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