Antiviral drug and preparation method therefor
A technology of pharmacy and derivatives is applied in the preparation of the antiviral drug, the esters of peramivir and plerixafor-N-alkanoic acid, and the derivative esters of peramivir, to achieve prolonging survival time, The effect of increased mortality protection
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Embodiment 1
[0047] Example 1 (1S, 2S, 3R, 4R)-1'-carboxylic acid-3'-[(1S)-1''-acetamido-2''-ethyl]butyl-4'-guanidino Cyclopenta-2'-oxo-{5-[1,4,8,11-tetraazacyclotetradecyl]methyl}phenyl)-1,4,8,11-tetraazacyclotetradecyl Alkyl]}-valerate
[0048]
[0049] (1) (1S,2S,3R,4R)-2-hydroxy-3-[(1S)-1-acetamido-2-ethyl]butyl-4-diBoc-guanidinocyclopentan-1- Benzyl carboxylate
[0050]
[0051] 32.8g (100mmol) of peramivir, 21.3g (112mmol) of p-toluenesulfonic acid, 54.1g (500mmol) of benzyl alcohol, add 500mL of toluene and reflux for 24 hours (using a water trap). After the reaction is complete, Add ethyl acetate to freeze crystallization, filter with suction, wash with ethyl acetate, add 200mL tetrahydrofuran to dissolve the filter cake, add 30.3g (300mol) of triethylamine, add 109.1g (500mmol) of di-tert-butyl dicarbonate (BOC anhydride) ), the reaction was stirred at room temperature for 24 hours. After the reaction was completed, 400 mL of dichloromethane was added, and the pH was adjusted to 2-...
Embodiment 2
[0067] Example 2 (1S, 2S, 3R, 4R)-1'-carboxylic acid-3'-[(1S)-1''-acetamido-2''-ethyl]butyl-4'-guanidino Cyclopenta-2'-oxo-{5-[1,4,8,11-tetraazacyclotetradecyl]methyl}phenyl)-1,4,8,11-tetraazacyclotetradecyl Alkyl]}-octadecanoate
[0068]
[0069] Prepared in the same manner as in Example 1, replacing ethyl 5-bromopentanoate in step (3) with ethyl 18-bromo-octadecanoate to obtain the target compound; high resolution mass spectrum (+ESI, m / z): 1096.6419 [M+H] + .
Embodiment 3
[0070] Example 3 (1S, 2S, 3R, 4R)-1'-carboxylic acid-3'-[(1S)-1''-acetamido-2''-ethyl]butyl-4'-guanidino Cyclopenta-2'-oxo-{5-[1,4,8,11-tetraazacyclotetradecyl]methyl}phenyl)-1,4,8,11-tetraazacyclotetradecyl Alkyl]}-methyl-phenyl-valerate
[0071]
[0072] Prepared as in Example 1, replacing 5-bromovalerate ethyl ester in step (3) with p-bromomethyl-phenylvalerate ethyl ester to obtain the target compound; high resolution mass spectrum (+ESI, m / z): 1004.4098 [M+H] + .
[0073] The following test examples are used to further compare and illustrate the selectivity index and death protection rate of peramivir derivative esters provided by the present invention.
PUM
Abstract
Description
Claims
Application Information
- R&D Engineer
- R&D Manager
- IP Professional
- Industry Leading Data Capabilities
- Powerful AI technology
- Patent DNA Extraction
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