Astragaloside derivative and preparation method and application thereof
A technology for a drug and methylamine, applied in the field of medicine, can solve the problems of many side reactions in the synthesis route, no prodrug properties, and two sugar chains are easy to fall off, so as to achieve improved druggability, less side reactions, and increased water solubility. Effect
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Image
Examples
Example Embodiment
[0026] Example 1
[0027] This example provides a method for preparing the compound with the structure of Formula 1 and its structure identification according to claim 1:
[0028] (1) Compound preparation: Take 100 mg of astragaloside IV, add it to 500 mL of 10% pyridine, add 25 mg of sodium bromide, 5 mg of 2,2,6,6-tetramethylpiperidine-1-oxy radical, 1mL of sodium hypochlorite, react at 0℃ for 120min, filter, and adjust the pH to 3 for the filtrate with concentrated hydrochloric acid. After the solid precipitates, concentrate to 20mL, separate solid and liquid, dissolve and transfer the solid with methanol, and concentrate to dryness to obtain 89.7mg of white powder. A compound having the structure of Formula 1 (HPLC purity 98.8%).
[0029] (2) Structure identification:
[0030] White amorphous powder; sprayed with 5% concentrated sulfuric acid / ethanol after TLC development, it shows purple red; (c, 1.0, MeOH); IR (KBr): Vmax: 3417, 2968, 1732, 1621, 1378, 1156, 1066, 1045cm -1 . ...
Example Embodiment
[0038] Example 2
[0039] This example provides a method for preparing the compound with the structure of Formula 1 according to claim 1. The difference compared with Example 1 is that the ratio of solvent and reagent is adjusted:
[0040] Take 100mg of astragaloside IV, add it to 50mL of water, add 25mg of sodium bromide, 10mg of 2,2,6,6-tetramethylpiperidine-1-oxy radical, 0.25mL of sodium hypochlorite, and react at 20℃ 120min, filter, adjust the pH of the filtrate with concentrated hydrochloric acid to 2, after the solids are separated out, concentrate to 10mL, separate the solids and liquids, dissolve and transfer the solids with ethanol, and concentrate to dryness to obtain 91.3mg of white powder, which is the compound with the structure of Formula 1 (HPLC purity 99.1%).
Example Embodiment
[0041] Example 3
[0042] This example provides a method for preparing the compound with the structure of Formula 1 according to claim 1. The difference compared with Example 1 is that the ratio of solvent and reagent is adjusted:
[0043] Take 100mg of astragaloside IV and add it to 10mL of 10% DMF, add 20mg of sodium bromide, 8mg of 2,2,6,6-tetramethylpiperidine-1-oxyl radical, and 0.20mL of sodium hypochlorite. React at ℃ for 120 min, filter, and adjust the pH to 3 with concentrated hydrochloric acid for the filtrate. After the solids are separated out, concentrate to 10mL, separate the solid and liquid, dissolve and transfer the solids with ethanol, and concentrate to dryness to obtain 82.7mg of white powder, which has the structure of formula 1. Compound (HPLC purity 97.9%).
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.
© 2023 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap