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Cefazolin derivative and its preparation method, oral antibiotic preparation

A technology for cefazolin and cefazolin acid, which is applied in the fields of cefazolin derivatives and their preparation, and oral antibiotic preparations, and achieves the effects of easily controllable reaction conditions, reduced incidence and good drug efficacy

Active Publication Date: 2016-06-29
SHENZHEN CHINA RESOURCES GOSUN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the above-mentioned deficiencies in the prior art, provide a kind of delicious cefazolin derivatives and preparation method thereof, to solve the technical problem that most of the existing antibiotics are water-soluble and use injection medicine

Method used

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  • Cefazolin derivative and its preparation method, oral antibiotic preparation
  • Cefazolin derivative and its preparation method, oral antibiotic preparation
  • Cefazolin derivative and its preparation method, oral antibiotic preparation

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preparation example Construction

[0024] Correspondingly, the present invention also provides a kind of synthetic method of above-mentioned cefazolin derivative, and this method comprises the steps:

[0025] S01. Prepare the mixed solution of the low-temperature reactant of cefazolin core and cefazolin acid: dissolve the cefazolin core and cefazolin acid in the reaction solvent and lower the temperature to below 5° C., then add a condensing agent to obtain Low temperature reactant mixed solution;

[0026] S02. Heating the low-temperature reactant solution for condensation reaction: heating the low-temperature reactant mixed solution prepared in step S01 to 20-30°C for condensation reaction, and after the reaction is completed, ice water is precipitated, solid-liquid separation, and purification treatment , to obtain the cefazolin derivative of the following molecular structural formula (I):

[0027]

[0028] Specifically, in the above-mentioned step S01, the purpose of dissolving the cefazolin mother nucle...

Embodiment 1

[0047] A kind of cefazolin derivative and its synthetic method

[0048] Cefazolin nuclei (3.4g) and cefazolin acid (4.5g) were dissolved in tetramethylguanidine (30ml), and the temperature was lowered to 0°C, and slowly added into the reaction solution and 1-ethyl-(3-di Methylaminopropyl) carbodiimide hydrochloride (2.2g), fully stirred to dissolve, the temperature was raised to 25°C, and the reaction was stirred for 12 hours; the reaction was stopped, and the reaction solution was poured into 1000ml of ice water, filtered to obtain a large amount of White solid, the filter cake was washed with sodium carbonate solution of pH7.5; the filter cake was dissolved in chloroform, separated by silica chromatography column to obtain 5.8 grams of cefazolin derivatives (formula I), with a purity of 99.3%. Its mass yield is 171%.

[0049] The cefazolin derivative prepared by the embodiment of the present invention 1 is carried out proton nuclear magnetic resonance spectrum analysis and ...

Embodiment 2

[0053] Cefazolin core (3.4g) and cefazolin acid (5.0g) were dissolved in tetramethylguanidine (100ml), and the temperature was lowered to 2°C, and slowly added to the reaction solution and 1-ethyl-(3-di Methylaminopropyl) carbodiimide hydrochloride (2.6g), fully stirred to dissolve, the temperature was raised to 22°C, and the reaction was stirred for 12 hours; the reaction was stopped, and the reaction liquid was poured into 1000ml of ice water, filtered to obtain a large amount of White solid, the filter cake was washed with sodium carbonate solution of pH7.8; the filter cake was dissolved in chloroform, separated by silica chromatography column to obtain 5.2 grams of cefazolin derivatives (formula I), with a purity of 99.5%. Its mass yield is 153%.

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Abstract

The invention discloses a cefazolin derivative and a preparation method thereof as well as an oral antibiotic preparation. The molecular structural formula of the cefazolin derivative is (I) shown in description. The preparation method comprises the following steps: preparing a low-temperature reactant mixed solution of a cefazolin mother nucleus and cefazolin acid and carrying out condensation reaction on the low-temperature reactant mixed solution through heating. The oral antibiotic preparation contains the cefazolin derivative with the structural formula (I). The cefazolin derivative disclosed by the invention has the activity of a cefazolin medicine, has a suitable lipid-water partition coefficient and is suitable for gastro-intestinal tract dosing. The preparation method has easily-controlled reaction conditions, a simple process and a high product yield. The oral antibiotic preparation has a good efficacy, is convenient and safe to use, and can effectively reduce the occurrence rate of abusing antibiotics; meanwhile, the range of selecting the oral antibiotic preparation in China is expanded.

Description

technical field [0001] The invention belongs to the technical field of antibiotic drugs, and in particular relates to a cefazolin derivative, a preparation method thereof and an oral antibiotic preparation. Background technique [0002] Infectious diseases are the most common clinical diseases and one of the most common causes of death in patients. According to the World Health Organization report 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 my country, due to the rapid growth of the total population, the acceleration of the aging process, the increase and accumulation of immunosuppressive hosts, the deterioration of the ecological environment, the increase of population mobility, the imbalance of social and economic development, and the frequent occurrence of famines, and With the vast rural population and the still backward medical security system, the main diseases that endanger people's ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D519/06C07D501/36C07D501/06A61K9/20A61P31/04
CPCC07D519/06
Inventor 黄权华蒋雄杰张远杏苏军权吴海华
Owner SHENZHEN CHINA RESOURCES GOSUN PHARMA CO LTD
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