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Orbifloxacin synthesis method

A technology for orbifloxacin and a synthesis method, which is applied in the direction of organic chemistry and the like, can solve problems such as no need for poultry diseases, and achieve the effects of short reaction time, high product yield and low reaction cost.

Active Publication Date: 2015-08-05
ZHENGZHOU BARY ANIMAL PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The drug is used abroad as a specific drug for treating pneumonia and diarrhea in livestock such as pigs and cattle, but not for treating poultry diseases

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] (1) tetrafluoroboric acid

[0024] In a 500ml three-necked flask, add 36 grams (0.6mol) of boric acid and 115ml of hydrofluoric acid (mass concentration 25%), and stir at 25°C to completely dissolve the boric acid in the hydrofluoric acid to prepare tetrafluoroboric acid for later use.

[0025] (2) Diazotization reaction

[0026] In a 500ml three-neck flask, add 156.8 grams (0.4mol) of sparfloxacin, 105ml of aqueous hydrochloric acid solution with a mass concentration of 30%, and slowly add 50ml of 12mol / L sodium nitrite aqueous solution dropwise under the cooling condition of 0-5°C ice-salt bath (0.6mol), stirred vigorously, and tested the end point of diazotization reaction with starch potassium iodide test paper to obtain a diazonium salt solution.

[0027] (3) preparation of sparfloxacin borofluoride

[0028] Add the tetrafluoroboric acid cooled to 0°C prepared in step (1) dropwise to the diazonium salt solution in step (2). Washed with ether and dried in vacuum ...

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Abstract

The present invention discloses an orbifloxacin synthesis method, which comprises: adopting sparfloxacin as a raw material, carrying out a diazotization reaction under the effect of hydrochloric acid and sodium nitrite to obtain a diazonium salt solution, adding tetrafluoroboric acid to the diazonium salt solution in a dropwise manner, carrying out a fluorization reaction at a temperature of -10 DEG C, filtering the reaction solution after completing the reaction, taking the filter cake, washing with ethyl ether, drying, heating the dried product until no gas is generated to obtain an orbifloxacin crude product, and purifying the orbifloxacin crude product to obtain the orbifloxacin. According to the present invention, the sparfloxacin is utilized as the starting raw material and the diazotization reaction and the fluorization reaction are used to prepare the orbifloxacin, such that advantages of new process route, high product yield, low reaction cost and short reaction time are provided, and the method is the new economical and practical technology.

Description

(1) Technical field [0001] The invention relates to a synthesis method of orbifloxacin, in particular to a method for preparing orbifloxacin from sparfloxacin through diazotization and fluorination reactions. (2) Background technology [0002] Obifloxacin is a third-generation fluoroquinolone-specific antibacterial drug for animals. The drug is used abroad as a specific drug for treating pneumonia and diarrhea in livestock such as pigs and cattle, but it is not used for treating poultry diseases. The bioavailability of orbifloxacin is as high as 89-100%, which is higher than that of enrofloxacin and danofloxacin, and the pharmacokinetic parameters of clinical application are significantly better than those of enrofloxacin and danofloxacin, especially the peak drug concentration The aging area of ​​the drug is much larger than the latter two, but the elimination half-life and drug withdrawal period are shorter than the latter two, and the absorption and tissue penetration ar...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04
CPCC07D401/04
Inventor 孙莉裴文王海滨杨振平
Owner ZHENGZHOU BARY ANIMAL PHARMA
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