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

Application and preparation method of benzo alpha-pyrone compounds

A technology of pyrone and compound, which is applied in the field of use of active ingredients of traditional Chinese medicine, and can solve problems such as non-research

Active Publication Date: 2014-01-08
SUN YAT SEN UNIV
View PDF0 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, benzoα-pyrone compounds are mostly used in the preparation of anticoagulant drugs, and the benzoα-pyrone compounds of the present invention have no research as PDE4 inhibitors

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
  • Application and preparation method of benzo alpha-pyrone compounds
  • Application and preparation method of benzo alpha-pyrone compounds
  • Application and preparation method of benzo alpha-pyrone compounds

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: the preparation of dragon's palm blood extract

[0026] Take 1 kg of the blood root of Feilongzhang, grind it into a coarse powder, add 8 times the volume of 95% ethanol to soak, ultrasonically extract 3 times, each time for 7 days, filter, combine the filtrates, recover ethanol under reduced pressure, and concentrate the remaining liquid to relative A thick ointment with a density of 1.25, containing 85g of the ethanol extract of Dragon Palm Blood.

Embodiment 2

[0027] Embodiment 2: the preparation of dragon's palm blood extract

[0028] The ethanol extract of Feilongzhangxue was sequentially extracted 3 times with 4 volumes of petroleum ether and ethyl acetate respectively, and the ethyl acetate extracts were combined and evaporated to dryness under reduced pressure to obtain 63 g of ethyl acetate extract.

Embodiment 3

[0029] Embodiment 3: Preparation of known monomeric compounds of benzo α-pyrone

[0030] (1) Take 1 kg of blood root of Feilong palm, pulverize it into a coarse powder, add 8 times the volume of 95% ethanol to soak, ultrasonically extract 3 times, each time for 7 days, filter, combine the filtrate, recover ethanol under reduced pressure, and the remaining liquid Concentrate to a thick paste with a relative density of 1.25 to obtain 85 g of the ethanol extract of Feilongzhang blood.

[0031] (2) The ethanol extract of Feilongzhang blood was sequentially extracted three times with 4 volumes of petroleum ether and ethyl acetate respectively, and the ethyl acetate extracts were combined and evaporated to dryness under reduced pressure to obtain 63 g of ethyl acetate extract.

[0032] (3) The ethyl acetate extract should be initially segmented by MCI column, and eluted with methanol: water = 3:7 ~ 10:0; then use 200-300 mesh column chromatography silica gel to use petroleum ether: ...

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

The invention discloses an application and a preparation method of a benzo alpha-pyrone compounds (the structures are shown in the specification). The preparation method comprises the following steps: crushing Toddaliaasiatica root, extracting the Toddaliaasiatica root through 95% ethanol, sequentially extracting the extract through petroleum ether and ethyl acetate to obtain two parts, and then, separating a series of benzo alpha-pyrone monomeric compounds from ethyl acetate extract through such separation measures as silica gel column chromatography, gel column chromatography, MCI column chromatography, ODS column chromatography, high performance liquid chromatography, and the like; the compounds obtained by the preparation method disclosed by the invention are 4 type phosphodiesterase (PDE4) inhibitors, thereby providing lead compounds for research and development of anti-inflammatory agents and anti-asthmatic drugs and capable of being used for preparing drugs for treating such inflammatory diseases as asthma or allergic rhinitis, etc.

Description

technical field [0001] The invention relates to a benzoα-pyrone compound, its application in medicine for treating diseases related to type 4 phosphodiesterase and its preparation method, and belongs to the field of active ingredients of traditional Chinese medicine. Background technique [0002] Cyclic nucleotide phosphodiesterases (PDEs) are an important family of super enzymes, through the hydrolysis of cAMP and cGMP, effectively control the concentration of cAMP and cGMP in cells, thereby regulating the transmission of second messengers in the body biochemical effect. PDEs are widely distributed in mammalian tissues, and their diversity leads to specific distribution of different PDE enzymes at the cellular and subcellular levels, which can selectively regulate a variety of cellular functions, and are good drug design and therapeutic targets. [0003] Phosphodiesterase type 4 (PDE4), as a PDE family enzyme that specifically catalyzes the hydrolysis of cAMP, is mainly di...

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
IPC IPC(8): A61K31/37A61P11/06A61P29/00A61P11/02
Inventor 尹胜罗海彬林婷婷黄仪有
Owner SUN YAT SEN UNIV
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