Preparation method of moxifloxacin hydrochloride and intermediate thereof

A technology for moxifloxacin hydrochloride and intermediates is applied in the field of preparation of moxifloxacin hydrochloride and intermediates thereof, and can solve the problems of unsuitability for industrial production, poor product purity and high production cost

Active Publication Date: 2018-12-28
上海新礼泰药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] The technical problem to be solved by the present invention is to provide a kind of moxifloxacin hydrochloride in order to overcome the defects such as the low yield of the preparation method of moxiflox

Method used

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  • Preparation method of moxifloxacin hydrochloride and intermediate thereof
  • Preparation method of moxifloxacin hydrochloride and intermediate thereof
  • Preparation method of moxifloxacin hydrochloride and intermediate thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Embodiment 1: the preparation of moxifloxacin hydrochloride intermediate II

[0064]

[0065] Under nitrogen protection, 10.0Kg (33.87 mol) and 7.95Kg (89.19mol) of 2-amino-2-methyl-1-propanol, heated to 105-115°C and refluxed for 6-7 hours and separated the produced water until it reached the measured amount or no longer increased . Cool to 10 ℃~20 ℃, add mass concentration successively respectively and be 2% acetic acid aqueous solution (the described mass concentration refers to the percentage that the quality of acetic acid accounts for the total mass of the acetic acid aqueous solution), and the mass concentration is 5% sodium carbonate aqueous solution (the described Mass concentration refers to the quality of sodium carbonate accounts for the percentage of the total mass of sodium carbonate aqueous solution), mass concentration is 7% sodium bicarbonate aqueous solution (described mass concentration refers to the quality of sodium bicarbonate accounts for the ...

Embodiment 2

[0066] Embodiment 2: the preparation of moxifloxacin hydrochloride intermediate II

[0067]Under nitrogen protection, 50.0 g (0.169 mol) and 60.4 g (0.678 mol) of 2-amino-2-methyl-1-propanol, heated to 75-85° C. and refluxed for 12-14 hours and separated the produced water. Cool to 10 ℃~20 ℃, add mass concentration successively respectively and be 2% acetic acid aqueous solution (the described mass concentration refers to the percentage that the quality of acetic acid accounts for the total mass of the acetic acid aqueous solution), and the mass concentration is 5% sodium carbonate aqueous solution (the described Mass concentration refers to the quality of sodium carbonate accounts for the percentage of the total mass of sodium carbonate aqueous solution), mass concentration is 7% sodium bicarbonate aqueous solution (described mass concentration refers to the quality of sodium bicarbonate accounts for the percent of the total mass of sodium bicarbonate aqueous solution) , mas...

Embodiment 3

[0068] Embodiment 3: the preparation of moxifloxacin hydrochloride intermediate II

[0069] Under nitrogen protection, 20.0 g of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acid was added to 150 mL of ethylbenzene ( 0.0677mol) and 10.9g (0.122mol) of 2-amino-2-methyl-1-propanol, heated to 130°C to 140°C and refluxed for 3 hours to 4 hours and separated the produced water. Cool to 10 ℃~20 ℃, add mass concentration successively respectively and be 2% acetic acid aqueous solution (the described mass concentration refers to the percentage that the quality of acetic acid accounts for the total mass of the acetic acid aqueous solution), and the mass concentration is 5% sodium carbonate aqueous solution (the described Mass concentration refers to the quality of sodium carbonate accounts for the percentage of the total mass of sodium carbonate aqueous solution), mass concentration is 7% sodium bicarbonate aqueous solution (described mass concentration ...

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Abstract

The invention discloses a preparation method of moxifloxacin hydrochloride and an intermediate thereof. The preparation method of the intermediate III of the moxifloxacin hydrochloride includes the following steps: making an intermediate II of the moxifloxacin hydrochloride and (S,S)-2,8-diazabicyclo[4,3,0]nonane have condensation reaction in an organic solvent in the presence of alkali to obtainthe intermediate III of the moxifloxacin hydrochloride. The preparation method is simple and safe in operation, does not require special equipment and avoids use of highly toxic materials and mild inreaction conditions. The obtained the moxifloxacin hydrochloride I has high purity and low production cost, and is suitable for industrial production. (img file='DDA0001750656940000011.TIF' wi='700' he='192'/).

Description

technical field [0001] The invention relates to a preparation method of moxifloxacin hydrochloride and an intermediate thereof. Background technique [0002] Moxifloxacin Hydrochloride (Moxifloxacin Hydrochloride, I) is a broad-spectrum and 8-methoxyfluoroquinolone antibacterial drug with antibacterial activity. Its indications are for the treatment of respiratory and lower respiratory tract infections, such as: acute sinusitis, acute chronic bronchitis outbreaks, community-acquired pneumonia, and skin and soft tissue infections. [0003] Moxifloxacin has shown broad-spectrum antibacterial activity in vitro against Gram-positive bacteria, Gram-negative bacteria, anaerobes, acid-fast bacteria, and atypical microorganisms such as Mycoplasma, Chlamydia, and Legionella. The antibacterial mechanism is to interfere with Ⅱ, Ⅳ topoisomerase. Topoisomerases are key enzymes that control DNA topology and are involved in DNA replication, repair and transcription. Its bactericidal cur...

Claims

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Application Information

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IPC IPC(8): C07D471/04
CPCC07D471/04
Inventor 陈健邹宝勤刘振峰应述欢
Owner 上海新礼泰药业有限公司
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