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Preparation method of lomefloxacin aspartate

A technology of lomefloxacin aspartate and lomefloxacin hydrochloride, which is applied in the field of preparation of lomefloxacin aspartate, can solve the problems of high cost of ethanol, and achieve the effects of avoiding health, saving resources, and promoting the use

Inactive Publication Date: 2016-09-21
河南精康制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the salt-forming reactions in the prior art all react in ethanol aqueous solution, and the cost of ethanol is relatively high, so it is imperative to improve the preparation process of lomefloxacin aspartate

Method used

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Embodiment 1

[0011] A preparation method of lomefloxacin aspartate, the preparation method of lomefloxacin aspartate comprises the following steps: a, neutralization reaction: taking lomefloxacin hydrochloride and potassium hydroxide in a molar ratio of 1 : 1 of lomefloxacin hydrochloride and potassium hydroxide aqueous solution for subsequent use, take by weighing 600 times the water of lomefloxacin hydrochloride molar number and add in the reaction kettle, add the standby lomefloxacin hydrochloride by weighing and stir, heat up to 60 ℃ to make the hydrochloric acid Lomefloxacin is completely dissolved in water, slowly start to drop potassium hydroxide aqueous solution, adjust the pH value of the solution to 7, keep warm and react for 2 hours, after the reaction is completed, the reaction solution is cooled to normal temperature; Centrifuge the material with the reaction solution, and use water to rinse until there is no chloride ion in the filtrate to obtain the wet product of lomefloxaci...

Embodiment 2

[0016] A preparation method of lomefloxacin aspartate, the preparation method of lomefloxacin aspartate comprises the following steps: a, neutralization reaction: taking lomefloxacin hydrochloride and sodium hydroxide in a molar ratio of 1 : 1.1 of lomefloxacin hydrochloride and sodium hydroxide aqueous solution for subsequent use, take by weighing 800 times the water of lomefloxacin hydrochloride molar number and add in the reaction kettle, add and take by weighing spare lomefloxacin hydrochloride and stir, heat up to 80 ℃ to make hydrochloric acid Lomefloxacin is completely dissolved in water, slowly drips aqueous potassium hydroxide solution, adjusts the pH value of the solution to 8, and insulates and reacts for 1 hour. After the reaction is completed, the reaction solution is cooled to normal temperature; Centrifuge the material with the reaction solution, and use water to rinse until there is no chloride ion in the filtrate to obtain the wet product of lomefloxacin base; ...

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Abstract

The invention relates to a preparation method of an anti-infectious agent, particularly relates to a preparation method of lomefloxacin aspartate. The preparation method comprises the steps of performing a neutralization reaction on lomefloxacin hydrochloride, water and an alkaline solution in proportion, obtaining lomefloxacin base, performing a salt forming reaction on the lomefloxacin base generated by the neutralization reaction, L-aspartate and the water in proportion, obtaining a lomefloxacin aspartate wet product, refining the lomefloxacin base, the L-aspartate and mother liquor obtained by a purified water salt forming reaction, obtaining the lomefloxacin aspartate wet product, and finally drying the lomefloxacin aspartate wet product, so as to obtain a finished product, generally, the preparation method has the advantages that the lomefloxacin aspartate can react in the water, the production cost can be effectively reduced, the reaction speed can be improved, the safety in the production process can be improved, the economic benefit of enterprise can be improved, and a high use value can be realized.

Description

technical field [0001] The invention relates to a preparation method of an anti-infective drug, in particular to a preparation method of lomefloxacin aspartate. Background technique [0002] Lomefloxacin is the third-generation quinolone antibacterial drug, which has a broad-spectrum antibacterial effect on Gram-negative bacteria and positive bacteria including Pseudomonas aeruginosa. Its salts are commonly used in the treatment of biliary tract, intestinal tract, skin and soft tissue infections, otitis media, and sinusitis. Lomefloxacin Aspartate (Lomefloxacin Aspartate) is its organic acid salt. Compared with common inorganic acid salts such as lomefloxacin hydrochloride, it is less irritating to the human body and better tolerated by patients. However, the salt-forming reactions in the prior art all react in ethanol aqueous solution, and the cost of ethanol is relatively high, so it is imperative to improve the preparation process of lomefloxacin aspartate. Contents of...

Claims

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Application Information

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IPC IPC(8): C07D401/04C07C227/18C07C229/24
CPCC07D401/04
Inventor 李怀生李东倡武玄之伊文峰
Owner 河南精康制药有限公司
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