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Preparation method of levofloxacin hydrochloride

A technology of levofloxacin hydrochloride and levofloxacin carboxylic acid, which is applied in the field of pharmaceutical preparation, can solve the problems of low purity of levofloxacin hydrochloride, long process flow, and difficult operation, etc., and achieve the effects of shortening the process cycle, avoiding high temperature conditions, and reducing energy consumption

Inactive Publication Date: 2017-05-17
HENAN KANGDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The synthesis process in the prior art has the following problems: 1) It is necessary to prepare levofloxacin crystals first, and then form a salt with hydrochloric acid. The prepared levofloxacin hydrochloride has low purity and needs to be refined again

Method used

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  • Preparation method of levofloxacin hydrochloride

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Effect test

Embodiment 1

[0030] A preparation method of levofloxacin hydrochloride, comprising the following steps;

[0031] 1) Mix and dissolve 50 g of levofloxacin, 100 g of N-methylpiperazine and 30 g of dimethyl sulfoxide, then stir and raise the temperature in a water bath to 80°C for 7 hours, then recover dimethyl sulfoxide under reduced pressure to dryness , lower the dry matter to room temperature and add 400g of chloroform and 100g of water to stir, and adjust the pH value to 7.0 with ammonia water, and separate the layers after standing still for 1 hour, discard the water layer, take the chloroform layer and add 75g of water, wash thoroughly for 30 minutes, and then separate the layers , take the chloroform layer and back-extract the water layer with 50 g of chloroform and incorporate it into the obtained chloroform layer, then distill the chloroform layer under normal pressure to dryness, and then distill it under reduced pressure to a solid powder.

[0032] 2) Add 60g of purified water to ...

Embodiment 2

[0034] A preparation method of levofloxacin hydrochloride, comprising the following steps;

[0035] 1) Mix and dissolve 50g of levofloxacin, 85g of N-methylpiperazine and 30g of dimethyl sulfoxide, then stir and raise the temperature in a water bath to 85°C for 6 hours, then recover dimethyl sulfoxide under reduced pressure to dryness , lower the dry matter to room temperature and add 400g of chloroform and 100g of water to stir, and adjust the pH value to 7.0 with ammonia water, and separate the layers after standing for 1 hour, discard the water layer, take the chloroform layer and add 100g of water, wash thoroughly for 30 minutes, and then separate the layers , take the chloroform layer and back-extract the water layer with 50 g of chloroform and incorporate it into the obtained chloroform layer, then distill the chloroform layer under normal pressure to dryness, and then distill it under reduced pressure to a solid powder.

[0036] 2) Add 60g of purified water to the solid...

Embodiment 3

[0038] A preparation method of levofloxacin hydrochloride, comprising the following steps;

[0039] 1) Mix and dissolve 50g of levofloxacin, 85g of N-methylpiperazine and 30g of dimethyl sulfoxide, then stir and raise the temperature in a water bath to 90°C for 8 hours, then recover dimethyl sulfoxide under reduced pressure to dryness , lower the dry matter to room temperature and add 400g of chloroform and 110g of water to stir, and adjust the pH value to 7.0 with ammonia water, and separate the layers after standing still for 1 hour, discard the water layer, take the chloroform layer and add 80g of water, wash fully for 30 minutes, and then stand still for layering , take the chloroform layer and back-extract the water layer with 60 g of chloroform and incorporate it into the obtained chloroform layer, then distill the chloroform layer under normal pressure to dryness, and then distill it under reduced pressure to a solid powder.

[0040] 2) Add 60g of purified water to the ...

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Abstract

The invention belongs to the technical field of medicine preparation, and in particular relates to a preparation method of levofloxacin hydrochloride, comprising the following steps: condensing levofloxacin carboxylic acid with N-methylpiperazine in a solvent; and acidifying the condensate with hydrochloric acid to obtain levofloxacin hydrochloride. In the method disclosed by the invention, levofloxacin condensed under the action without a catalyst and hydrochloric acid directly perform salt-forming reaction, so that the technical process is shortened, the reaction conditions have mildness and strong controllability, the content of a product external standard method can reach high than 91.0%, and the yield can reach 122-130%.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, in particular to a preparation method of levofloxacin hydrochloride. Background technique [0002] Levofloxacin Hydrochloride is the left-handed form of ofloxacin, and its antibacterial activity is about twice that of ofloxacin. Its main mechanism of action is to inhibit the activity of bacterial DNA gyrase (bacterial topoisomerase II), Blocks bacterial DNA replication. [0003] Levofloxacin hydrochloride is suitable for genitourinary system infections caused by sensitive bacteria, including simple and complicated urinary tract infections, bacterial prostatitis, Neisseria gonorrhoeae urethritis or cervicitis (including those caused by enzyme-producing strains). Respiratory tract infection, including acute attack of bronchial infection and lung infection caused by sensitive gram-negative bacilli. Gastrointestinal infection, caused by Shigella, Salmonella, enterotoxigenic Escherichia...

Claims

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Application Information

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IPC IPC(8): C07D498/06
CPCC07D498/06
Inventor 李文杰曹文英高德瀛安丽平刘红坤孟源
Owner HENAN KANGDA PHARMA
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