Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Preparation method of antiviral drug mupiravir

A technology of antiviral drugs and compounds, which is applied in the field of medicine and chemical industry, can solve the problems of low reaction yield, excessive three wastes, and high process cost, and achieve the effect of improving route efficiency, reducing three wastes, and increasing yield

Pending Publication Date: 2022-04-08
ANHUI HAIKANG PHARMA
View PDF1 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The biggest problem with this route is that the yield of the two-step key reaction is too low and there are more three wastes, the process cost is too high, and it is not suitable for scale-up production

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation method of antiviral drug mupiravir
  • Preparation method of antiviral drug mupiravir
  • Preparation method of antiviral drug mupiravir

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0046] Method for preparing an antiviral drug Morave: The preparation method comprises the following steps:

[0047] S1, synthetic compound 2:

[0048] The compound 1 cytosine was put into the reaction vessel, and the compound 1 cytidine was raw material;

[0049] The solution 1 was added to the reaction vessel for replacement, and then the protective group DMF-DMA was added three times;

[0050] The reaction system was warmed, and the dissolution reaction was stirred under a nitrogen atmosphere. When the TLC showed the compound 1 reaction, the intermediate 1 was obtained; the reaction solvent in the solution 1 was used in dichloromethane, toluene, tetrahydrofuran, methanol, ethanol, and pyridine. Any one; the reaction temperature of this step is -1-90 ° C, the reaction time is 1-15 h; the chemical name of the protecting base DMF-DMA is: N, N-dimethylformamide dimethylhyset;

[0051] The intermediate 1 was subjected to pressure reduction distillation treatment to obtain Compound 2...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

A preparation method of an antiviral drug mupiravir comprises the following steps: S1, synthesizing a compound 2: putting a compound 1 cytidine into a reaction container, and taking the compound 1 cytidine as a raw material; adding the solution 1 into the reaction container for replacement, and adding a protecting group DMF-DMA after three times of replacement; s2, synthesizing a compound 3; S3, synthesizing a compound 4; S4, synthesizing Molnupiravir: adding a solution 4 into a reaction system of the compound 4; the solution 4 comprises a reaction solvent and hydroxylamine sulfate; adding a pulping solvent into the intermediate 4, heating to 50 DEG C, and pulping for 30 minutes to obtain a product Molnupiravir; according to the preparation method, cytidine is taken as a starting raw material, DMF-DMA protecting groups are added, then esterification reaction, protecting group removal and hydroxyamination reaction are sequentially performed, a five-step one-pot method is realized, the route efficiency is effectively improved, the yield is increased, generation of three wastes is also effectively reduced, and the Molnupiravir with relatively high purity is obtained by finally purifying the system.

Description

Technical field [0001] The present invention belongs to the field of pharmaceutical chemical technology, and more particularly to the preparation method for maprave for antiviral oral propylene cytidine drugs. Background technique [0002] Moiriwell English is named molnupiravir, code number MK-448 or EIDD-2801, is chemically called: (2R, 3S, 4R, 5R) -3,4-dihydro-5- (4- (hydroxylamine) -2-oxoprimidine-1 (2H) -yl) tetrahydrofuran-2-yl) methyl isobutyl ester, structural formula is as follows: [0003] [0004] Molnupiravir is a small tonion antiviral drug developed by the American Pharmaceutical Giant Mercure East. The drug is a SARS-COV2 polymerase inhibitor, and studies have confirmed that molnupiravir is used to treat SARS-COV-2 snow, which can effectively inhibit viruses and prevent new crown viruses within 24 hours. Thereby suppressing viral propagation. The research team believes that if Molnupiravir can also achieve similar effects in the human body test, then new crown pa...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/067C07H1/00C07H1/06A61P31/12
Inventor 钱明何亚奇吴飞飞
Owner ANHUI HAIKANG PHARMA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com