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Preparation process of moxifloxacin

A preparation process, moxifloxacin technology, applied in the field of moxifloxacin preparation process, can solve the problems of boron impurity difficult to remove, moxifloxacin purity and yield reduction, etc., to achieve the effect of high purity and yield

Active Publication Date: 2019-12-13
HARBIN ZHENBAO PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many ways to prepare moxifloxacin, one of which is to add catalyst (such as boric acid-acetic anhydride) and gaticarboxylic acid compounds, such as ethyl gaticarboxylate to form a chelate, and then with (S, S) -2,8-diazabicyclo[4,3,0]nonane reacts to form moxifloxacin. Although the conversion efficiency of this method is improved, the impurities containing boron formed by this method are difficult to remove, resulting in the final The purity and yield of moxifloxacin will decrease

Method used

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  • Preparation process of moxifloxacin
  • Preparation process of moxifloxacin
  • Preparation process of moxifloxacin

Examples

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preparation example Construction

[0039] The preparation technology of moxifloxacin comprises the following steps:

[0040] S1, synthesize MX-2;

[0041] First, synthesize MX-2 according to the following formula:

[0042]

[0043] Among them, the synthesis of MX-1 is a compound known to those skilled in the art, and its synthesis is also known to those skilled in the art, so the present invention will not describe it in detail.

[0044] Preferably, the synthesis includes: mixing and reacting MX-1, solvent, basic substance and (S,S)-2,8-diazabicyclo[4,3,0]nonane;

[0045] Preferably, the conditions of the synthesis reaction are: the temperature is 0-80°C, and the time is 30 minutes-20 hours;

[0046] More preferably, the temperature is 40-50° C. and the time is 1-1.5 hours.

[0047] Further, the molar ratio of MX-1 and alkaline substance is 1:0.2-3; more preferably 1:0.5-1;

[0048] Preferably, the alkaline substance is an amine substance, more preferably, triethylamine;

[0049] Preferably, the solvent...

Embodiment 1

[0084] The present embodiment provides a kind of preparation technology of moxifloxacin:

[0085] Prepare with reference to the following formula:

[0086]

[0087] Add 30.00g (0.073mol) MX-1 to a 500ml four-neck flask, add 74.5ml acetonitrile, stir until dissolved; slowly add 9.84g (0.075mol) (S,S)-2,8-diazabicyclo[4 ,3,0] nonane, triethylamine 10g (0.099mol), temperature control 45 ℃, stirring for 1.5 hours. Cool down to 0°C after the reaction and add cooling methanol-hydrochloric acid solution (74g (2.31mol) of methanol, 20.2g (0.204mol) of concentrated hydrochloric acid with a mass concentration of 37%)) and stir at 8°C for 10 minutes under temperature control, then add 20g of glycerol ( 0.217mol) and stirred for 10 minutes, added moxifloxacin with a purity of 99.5% as crystal form 2 as seed crystal, and stirred and grown the crystal for 1 hour, added acetone 108g (1.86mol) and continued stirring and grown the crystal for 3 hours; filtered and washed the filter cake wi...

Embodiment 2- Embodiment 9

[0089] Example 2-Example 9 Prepare moxifloxacin with reference to the preparation process provided in Example 1, the difference is that the specific operating conditions are different.

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Abstract

The invention relates to the technical field of pharmaceutical engineering, specifically to a preparation process of moxifloxacin. The preparation process comprises the following steps: carrying out ahydrolysis reaction on a moxifloxacin chelate which is chelated with borate so as to form a crude moxifloxacin product containing boric acid; subjecting polyol and the crude moxifloxacin product containing boric acid to a chelation reaction; and then adding a poor solvent for crystallization. The preparation process of the invention can effectively remove elemental boron in the crude moxifloxacinproduct, and the yield and the purity of prepared moxifloxacin are excellent.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical engineering, in particular to a preparation process of moxifloxacin. Background technique [0002] Moxifloxacin, a quinolone drug, is mainly used clinically to treat adults (≥18 years old) with upper and lower respiratory tract infections, such as: acute sinusitis, acute exacerbation of chronic bronchitis, community-acquired pneumonia, and skin and soft tissue infections. There are many ways to prepare moxifloxacin, one of which is to add catalyst (such as boric acid-acetic anhydride) and gaticarboxylic acid compounds, such as ethyl gaticarboxylate to form a chelate, and then with (S, S) -2,8-diazabicyclo[4,3,0]nonane reacts to form moxifloxacin. Although the conversion efficiency of this method is improved, the impurities containing boron formed by this method are difficult to remove, resulting in the final The purity and yield of moxifloxacin will be reduced. [0003] In view of this, ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04
CPCC07D471/04
Inventor 方同华闫久江王喜军韩冰石成
Owner HARBIN ZHENBAO PHARMA
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