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Peramivir intermediate 9 impurity F as well as preparation method and application thereof

A technology for intermediates and impurities, applied in the field of medicinal chemistry, can solve problems such as no relevant reports, and achieve the effect of ensuring drug safety

Pending Publication Date: 2021-01-26
天津应天成科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] During the impurity research process of peramivir, impurity F of peramivir intermediate 9 was found, and there was no relevant report about this impurity in other literatures

Method used

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  • Peramivir intermediate 9 impurity F as well as preparation method and application thereof
  • Peramivir intermediate 9 impurity F as well as preparation method and application thereof
  • Peramivir intermediate 9 impurity F as well as preparation method and application thereof

Examples

Experimental program
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Embodiment 1

[0032] Add 10g of peramivir intermediate 8 to 100mL of methanol, add 0.5g of platinum dioxide, and then add 1ml of concentrated hydrochloric acid, in a hydrogen atmosphere of 1Mpa, heat up to 20-30°C and stir for 3h, cool to room temperature, and replace with nitrogen , filtered, concentrated, and the obtained solid was prepared and separated to obtain the impurity F of the peramivir intermediate 9.

[0033] The peramivir intermediate 9 impurity F that obtains with embodiment 1 is that sample is carried out spectrum analysis

[0034] Peramivir intermediate 9 impurity FHPLC purity: 91.5%, see figure 1 ; [M+H]+ peak 359.26, see figure 2 , 1H-NMR see image 3 .

[0035] figure 1 The specific situation of the HPLC collection of illustrative plates is as follows:

[0036] name Peak time (min) Peak area Peak area(%) Peak height N / A 8.435 1.214 7.199 5.920 N / A 11.217 0.215 1.277 0.978 Impurity F 18.437 15.429 91.524 42.115

[00...

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Abstract

The invention provides a peramivir intermediate 9 impurity F. The structural formula of the peramivir intermediate 9 impurity F is shown as a formula (I). The preparation method of the peramivir intermediate 9 impurity F comprises the following steps: A, performing reduction reaction on a peramivir intermediate 8 and a reducing agent in an organic solvent and an acid solution at the reaction temperature of -20 DEG C to 100 DEG C for 2-10 hours to obtain a reaction solution; and B, concentrating the reaction solution under reduced pressure to obtain a crude product of the impurity F of the peramivir intermediate 9, and conducting purifying to obtain the impurity F of the peramivir intermediate 9. Through research on peramivir impurities, the brand-new peramivir intermediate 9 impurity F isobtained, through mass spectrometry, the MS has a [M+1] peak 359.26, the corresponding molecular weight is 358.25, the purity reaches 90.0% or above, the impurity F can be used as a reference substance for impurity research for peramivir content determination, and the medication safety of peramivir can be effectively guaranteed.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a peramivir intermediate 9 impurity F and a preparation method and application thereof. Background technique [0002] Peramivir, chemical name: (1S,2S,3S,4R)-3-[(S)-1-Acetamido-2-ethylbutyl]-4-guanidino-2-hydroxycyclopentane -1-Carboxylic acid; a neuraminidase inhibitor targeting the surface glycoprotein neuraminidase of influenza virus, the first neuraminidase inhibitor approved as a single intravenous injection . Peramivir is suitable for patients aged 18 years and above with acute uncomplicated influenza and only two days of flu symptoms. The existing clinical trial data proves that it is effective against influenza A and influenza B. [0003] According to the internationally recognized drug registration, it must meet the requirements of the International Council for Harmonization of Human Drug Registration Technology (ICH) and the European Pharmacopoeia, which...

Claims

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Application Information

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IPC IPC(8): C07C271/24C07C269/06C07C269/08G01N1/28
CPCC07C271/24C07C269/06C07C269/08G01N1/28C07C2601/08G01N2001/2893
Inventor 王艳锤丘忠丽李学东董东英王秀秀
Owner 天津应天成科技有限公司
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