Peramivir hydrate crystal, preparation method, medical compound and usage thereof

A technology of lamiver hydrate and hydrate, which is applied to the hydrate crystal of peramivir, the application field of medicine, and can solve the problems of difficulty in storage of anhydrous substances and the like.

Active Publication Date: 2014-07-09
TIANJIN INSTITUTE OF PHARMA RESEARCH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, peramivir has strong hygroscopicity, and it is difficult to store anhydrous matter.

Method used

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  • Peramivir hydrate crystal, preparation method, medical compound and usage thereof
  • Peramivir hydrate crystal, preparation method, medical compound and usage thereof
  • Peramivir hydrate crystal, preparation method, medical compound and usage thereof

Examples

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preparation example Construction

[0044] According to the peramivir hydrate crystal of the present invention, it contains 2.5 crystal waters. The stated amount of water of crystallization is a statistical value. Its preferred preparation method is as follows: (1) refining step: add peramivir crude product in methanol, heat to 80 ℃ for dissolving in distilled water, heat filtration, filtrate atmospheric pressure distillation, steam to boiling point 98 ℃, stop distillation, cool down to Stir at 25°C for 5 hours, filter, and wash with a small amount of water to obtain a white solid; (2) Vacuum drying step: put the white solid in a vacuum desiccator, add a desiccant to dry, vacuumize the system, and dry for more than 2 days to obtain paramilk Wei 2.5 Hydrate.

[0045] According to a further preferred embodiment of the present invention, the weight ratio of the peramivir crude product, methanol and distilled water is 1:2:4.5.

[0046]According to a more preferred embodiment of the present invention, the desiccant...

Embodiment 1

[0079] Embodiment 1, preparation of new crystals of peramivir 2.5 hydrate:

[0080] Add peramivir crude product in 5 liters of three-necked flasks (according to the method of publication number CN101538228A with (±) 2-azabicyclo [2.2.1] hept-5-en-3-one as starting material, implement according to CN101538228A Example 3, 9, 12, 14, 16) 600 grams, methanol (chemically pure reagent) 1500 milliliters, water 2700 milliliters. Heated to reflux temperature, stirred and dissolved, and filtered hot. The filtrate was distilled at normal pressure until the boiling point was 98°C, the distillation was stopped, the temperature was lowered to 25°C and stirred for 5 hours, filtered and washed with a small amount of water to obtain a white solid. Put the white solid in a vacuum desiccator, add anhydrous calcium chloride to dry, the system is evacuated (vacuum degree 0.08MPa), temperature is 25°C, and dried for more than 2 days. Obtain 579 grams of peramivir 2.5 hydrate crystals.

[0081]...

Embodiment 2

[0104] Embodiment 2, preparation of peramivir 2.5 hydrate new crystals:

[0105]Add 200 grams of peramivir crude product, 485 milliliters of methanol, and 900 milliliters of water in a 2-liter three-neck flask. Heated to reflux temperature, stirred and dissolved, and filtered hot. The filtrate was distilled at normal pressure until the boiling point was 98°C, the distillation was stopped, the temperature was lowered to 25°C and stirred for 5 hours, filtered and washed with a small amount of water to obtain a white solid. Put the white solid in a vacuum desiccator and dry it without adding phosphorus pentoxide at a temperature of 30°C. The system is vacuumed (vacuum degree 0.09MPa) and dried for more than 2 days. 174 grams of peramivir 2.5 hydrate crystals were obtained.

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Abstract

The invention provides a peramivir hydrate crystal, a preparation method for the crystal, a medical compound containing the crystal and the application of the crystal in preparing the drugs for resisting influenza virus. The structural formula of the peramivir is shown in the description.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry. Specifically, the present invention relates to a peramivir hydrate crystal, a preparation method, a pharmaceutical composition, and an application of the crystal in the preparation of a drug for inhibiting influenza virus neuraminidase. Background technique [0002] The main role of neuraminidase (NA) in influenza virus is to promote the separation and diffusion of newly formed virions from infected cells, and promote the diffusion of virions from infected respiratory mucosa to surrounding tissues. In addition, NA also has the functions of enhancing the toxicity of virus strains and causing apoptosis, leading to flu symptoms and respiratory inflammation. NA inhibitor drugs can inhibit the replication of influenza virus, reduce its pathogenicity, alleviate the symptoms of influenza, shorten the course of the disease, and reduce complications. At present, NA inhibitors include zanamivir, oselta...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C279/16C07C277/08A61K31/196A61P31/16
Inventor 张晓军韩学文范巧云李卫东王淑仙
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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