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Preparation method and application of peramivir related substances

A technology of related substances and reactions, applied in the field of preparation of peramivir related substances, can solve problems such as affecting the quality of medicines

Pending Publication Date: 2021-04-23
日照正济药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The starting materials, intermediates, reaction by-products, and degradation impurities in the synthesis of peramivir may become impurities remaining in the final product (peramivir), thereby affecting the quality of the drug
At present, there are few reports on the research on peramivir related substances and the research on quality control analysis methods

Method used

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  • Preparation method and application of peramivir related substances
  • Preparation method and application of peramivir related substances
  • Preparation method and application of peramivir related substances

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030]

[0031] 10.0g of the crude product of compound I-A was added to the reaction flask, then 70ml of toluene was added as a reaction solvent, then heated to 48-52°C, and 2.85g of acetic anhydride was added dropwise under temperature control within this temperature range, and the dripping was completed and maintained The temperature of the system was kept between 48-52 °C and the reaction was stirred. After the TLC monitored the disappearance of the raw material reaction, the reaction system was cooled to room temperature, washed once with an aqueous sodium chloride solution, left to stand for liquid separation, and the separated organic phase was then chlorinated again. The sodium aqueous solution was washed once, left to stand for separation, and the obtained organic phase was concentrated to dryness under reduced pressure to obtain 11.08 g of crude I-B.

[0032] The crude I-B was purified by column chromatography with 3% methanol-dichloromethane system to obtain 3.1 g ...

Embodiment 2

[0037] Liquid chromatographic analysis method for separation and determination of peramivir and its related substances (formula I)

[0038] Instrument: Agilent 1100 / 1260 High Performance Liquid Chromatograph

[0039] Column: Agilent Zorbax Bonus RP (250×4.6mm, 3.5μm)

[0040] Mobile phase: 10mmol / L dipotassium hydrogen phosphate solution (adjust the pH value to 4.5 with phosphoric acid) as mobile phase A, take mobile phase A-acetonitrile=40:60 as mobile phase B, and perform linear gradient elution as follows:

[0041]

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PUM

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Abstract

The invention discloses a preparation method and application of a peramivir related substance I. The related substance can be used as a peramivir impurity reference substance for separating and determining peramivir and the peramivir related substance I by a high performance liquid chromatography method. The preparation method provided by the invention has the advantages of mild reaction conditions and simple post-treatment, and can be used for large-scale preparation of the compound shown as the formula I with purity meeting the requirements to serve as an impurity reference substance for peramivir quality research.

Description

technical field [0001] The invention relates to a synthesis technology of pharmaceutical impurities, in particular to a preparation method and application of peramivir related substances. Background technique [0002] Peramivir is a novel cyclopentane anti-influenza virus drug. It is another new anti-influenza virus NA inhibitor after the successful development of oseltamivir and zanamivir and its launch in 1999. And as my country's first intravenous neuraminidase inhibitor and approved by the State Food and Drug Administration on April 5, 2013, the current clinical data show that it is effective against influenza A and B. The structural formula of peramivir is as follows: [0003] [0004] The quality control of APIs and preparations has always been the focus and difficulty in the process of drug research and development, and the research on impurities is the top priority in quality control. The starting materials, intermediates, reaction by-products, degradation impuri...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C277/08C07C279/16G01N30/02G01N30/34
CPCC07C269/06C07C231/12C07C277/08G01N30/02G01N30/34C07C2601/08C07C271/24C07C233/47C07C279/16
Inventor 罗林邹晓东胡锦亮郭辉赵佳楠
Owner 日照正济药业有限公司
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