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The synthetic method of favipiravir

A favipiravir and synthesis method technology, applied in the field of drug synthesis, can solve problems such as hydrogen peroxide aggregation and explosion, and achieve the effects of reducing pollution and loss, high production efficiency, and high mass transfer efficiency

Active Publication Date: 2022-08-02
苏州正济药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] WO2013180149A discloses that in 6-fluoro-3-hydroxyl-2-(5-D)pyrazinenitrile, add water, sodium hydroxide and 30% hydrogen peroxide aqueous solution, stir at room temperature for 15 minutes, and obtain 6-Fluoro-3-hydroxy-2-(5-D) pyrazine carboxamide, there is a risk of aggregation and explosion when a large amount of hydrogen peroxide is used in production

Method used

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  • The synthetic method of favipiravir
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  • The synthetic method of favipiravir

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Experimental program
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Effect test

Embodiment 1

[0035] A method for synthesizing favipiravir using a micromixer and a microchannel reactor in combination, the reaction flow is as follows figure 1 As shown, the reaction formula is as follows:

[0036]

[0037] Include the following steps:

[0038] 1. Prepare the solution:

[0039] Prepare 6-fluoro-3-hydroxypyrazine-2-carbonitrile (10g, 72mmol), sodium hydroxide (2.85g, 72mmol), 72ml of water (1mol / l), and mix the three reagents to prepare component A ;

[0040] Prepare hydrogen peroxide (16.3 g, 144 mmol), sodium hydroxide (2.85 g, 72 mmol), and 72 ml of water (1 mol / l), and prepare component B by mixing the three reagents.

[0041] 2. Set the injection pump parameters:

[0042] Set injection pump 1 (injection pump 1 is connected to solution A) injection rate, 25 degrees Celsius, 0-1Mpa,

[0043] Set the injection rate of the injection pump 2 (the injection pump 2 is connected to the solution B), 25 degrees Celsius, 0-1Mpa.

[0044] 3. Screening the Micromixer:

[...

Embodiment 2

[0051] The method for synthesizing favipiravir using DMSO solvent in combination with microchannel reactor, the reaction flow is as follows figure 2 As shown, the reaction formula is as follows:

[0052]

[0053] Include the following steps:

[0054] 1. Prepare the solution:

[0055] Component A: 10g of 6-fluoro-3-hydroxypyrazine-2-carbonitrile (1eq) and 5.8g of NaOH (2eq) were added with 5.6g of DMSO (1eq), and 90ml of water was mixed into a clear solution (C=0.8mol / l);

[0056] Component B: 16.5g H 2 O 2 (2eq).

[0057] 2. Set the injection pump parameters:

[0058] Set the injection pump 1 (the injection pump 1 is connected with solution A) 0.5ml / min, 25 degrees Celsius, 0-1Mpa.

[0059] Set the injection pump 2 (the injection pump 2 is connected with solution B) 0.1ml / min, 25 degrees Celsius, 0-1Mpa.

[0060] 3. Set the microchannel reactor parameters:

[0061] 35 degrees Celsius, 0-1Mpa, 5 modules, heart-shaped structure.

[0062] Table 3. The reaction condi...

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Abstract

The invention discloses a method for synthesizing favipiravir, which specifically comprises using DMSO in combination with a microchannel reactor, or a micromixer and a microchannel reactor, and is composed of 6-fluoro-3-hydroxy-2-cyanopyrazine in NaOH and H 2 O 2 Favipiravir was prepared under the conditions. The synthesis method of the present application uses a microchannel reactor, which has high mass transfer efficiency and can significantly improve the reaction conversion rate, thereby reducing pollution and loss; the method of the present application has a short reaction time, the entire reaction time is between 1-10 minutes, and the production efficiency is high; The continuous reaction is realized, the production efficiency is improved, and the labor cost is reduced. And because the reactant hydrogen peroxide is dangerous as an oxidant, the method has high safety.

Description

technical field [0001] The invention relates to a drug synthesis technology, in particular to a method for synthesizing favipiravir. Background technique [0002] Favipiravir (favipiravir, T-705, trade name Avigan, 1), chemical name 6-fluoro-3-hydroxy-2-pyrazinecarboxamide, is a targeted RNA-dependent drug developed by Japan's Toyama Chemical Pharmaceutical Company A novel broad-spectrum antiviral drug of RNA polymerase (RdRp) was approved for marketing in Japan in March 2014 for the treatment of novel and recurrent influenza. The mechanism of action of favipiravir is mainly that after entering the body, under the action of a series of cellular phosphokinases, it generates the form of its nucleoside analog triphosphate, thereby interfering with the replication and transcription of the virus. The study found that favipiravir has good inhibitory activity against various RNA viruses in vitro or in vivo, and is expected to be developed and applied to the treatment of various vi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D241/24B01J19/00
CPCC07D241/24B01J19/0093
Inventor 李小伟葛敏付明伟
Owner 苏州正济药业有限公司
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