Method for purifying pazufloxacin mesylate

A technology of pazufloxacin mesilate and pazufloxacin, which is applied in the field of preparation of pazufloxacin mesilate, can solve the problem that the quality of pazufloxacin mesilate cannot reach that of pazufloxacin mesilate Quality standard requirements and other issues, to achieve the effect of high economic and practical value, long shelf life and high purity

Inactive Publication Date: 2010-12-29
ZHEJIANG STARRY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, the quality of pazufloxacin mesylate obtained by the above two me

Method used

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  • Method for purifying pazufloxacin mesylate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Add pazufloxacin mesylate (10 g) and N,N-dimethylacetamide (45 mL) into a 100 mL single-necked bottle, heat to an internal temperature of 120° C. under electromagnetic stirring, and dissolve completely. Naturally lowered to room temperature, cooled to 0°C, and left overnight. Filter, wash the filter cake with ethanol (3x15mL), and vacuum-dry at 60°C for 12 hours to obtain 7.5g of pazufloxacin mesylate (purification rate: 75%).

Embodiment 2

[0043] Add pazufloxacin mesylate (10g) and N,N-dimethylacetamide (20mL) into a 100mL single-necked bottle, heat to 60°C, dissolve; cool to 0°C, stand overnight; filter, wash with 5mL ethanol Washing, repeated washing for a total of 3 times, vacuum drying at 50°C for 10 hours to obtain the refined product of pazufloxacin mesylate.

Embodiment 3

[0045]Add 10g of pazufloxacin mesylate and 200ml of N,N-dimethylacetamide into a 500mL single-necked bottle, heat to 135°C, dissolve; cool to 10°C, leave overnight; filter, wash with 50mL of ethanol, repeat washing A total of 3 times, vacuum drying at 105°C for 24 hours to obtain the refined product of pazufloxacin mesylate.

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Abstract

The invention relates to a method for preparing pure pazufloxacin mesylate. The method comprises the step of treating the pazufloxacin mesylate or pazufloxacin by using N,N-dimethyl acetamide.

Description

technical field [0001] The invention relates to a preparation method of a pharmaceutical compound, in particular to a preparation method of pazufloxacin mesylate, and the pazufloxacin mesylate injection is widely used in the clinical treatment of various bacterial infections. technical background [0002] Pazufloxacin mesylate is a new type of quinolone antibacterial agent for injection jointly developed by Japan Toyama Chemical Co., Ltd. and Japan Mitsubishi Pharmaceutical Co., Ltd. It was first launched in Japan in April 2002. Its chemical name is (S)-10-(1-aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3 -de][1,4]benzoxazine-6-carboxylic acid methanesulfonate, chemical structural formula (I): [0003] [0004] Pazufloxacin mesylate belongs to the fourth generation of quinolone antibacterial agents. This product has less toxicity to the central nervous system, its activity against Staphylococcus aureus is better than that of levofloxacin and cipro...

Claims

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Application Information

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IPC IPC(8): C07D498/06
Inventor 李奇彪张鹏顾洪霞王哲
Owner ZHEJIANG STARRY PHARMA
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