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

Propofol derivative for therapy

A technology of compounds and hydrates, which is applied to compounds of elements of group 5/15 of the periodic table, drug combinations, phosphorus organic compounds, etc., can solve problems such as low bioavailability and limit treatment development, and achieve good solubility effects

Inactive Publication Date: 2010-07-21
HC SYNTHETIC PHARMA CO LTD
View PDF4 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the low bioavailability of propofol when administered by means other than the intravenous route has limited the development of such treatments

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
  • Propofol derivative for therapy
  • Propofol derivative for therapy
  • Propofol derivative for therapy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Embodiment 1: the preparation of compound A

[0049] Dissolve 1.78g of propofol in 20ml of acetonitrile, slowly add 3ml of phosphorus oxychloride solution dropwise at room temperature, after the drop is complete, stir and react at room temperature for 5 hours, slowly add ice water and stir for hydrolysis reaction for 2 hours, evaporate to dryness under reduced pressure Solvent, dissolved in 30ml of tetrahydrofuran, added 3g of serine whose amino group was protected by BOC and carboxyl group by benzyl group, added 2g of triphenylphosphine, slowly added dropwise 2ml of diethyl azodicarboxylate solution, reacted at room temperature for 5 hours, and the reaction was completed , evaporated to dryness under reduced pressure, added ethyl acetate 50ml to dissolve, filtered the insoluble matter, purified by chromatography (eluting with ethyl acetate / n-hexane from n-hexane to 10%) the crude product, combined the filtrates, evaporated to dryness, and then used 30 % trifluoroacetic...

Embodiment 2

[0050] Example 2: Preparation of Compound B.

[0051] It was prepared according to the method of Embodiment 1 except that propofol was replaced by O-(hydroxymethyl)-2,6-diisopropylphenol.

Embodiment 3

[0052] Example 3: Preparation of Compound C.

[0053] Prepared according to the method of Example 1 except that succinoyl chloride was used instead of phosphorus oxychloride.

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 provides a propofol derivative as well as a preparation method and purpose thereof. The propofol derivative is obtained by chemically modifying the hydroxyl group in the structure of propofol. The related propofol derivative can be used in pharmaceutical composition and can be used for producing medicaments for anaesthesia.

Description

Technical field: [0001] The present invention relates to a propofol derivative used for treatment, its preparation method and application. technical background: [0002] During the last 15 years of anesthesia therapy, the use of injectable anesthetics, especially propofol, for the induction and maintenance of general anesthesia has gained wide acceptance. Intravenous anesthesia with propofol has several advantages over previous methods: such as a more tolerable induction because the patient does not have to worry about wearing a mask, suffocation, or the strong odor of the volatile anesthetic; rapid and predictable recovery; The dose of pofol is easy to adjust the depth of anesthesia; it has a low incidence of adverse reactions compared with inhalation anesthetics; it has reduced anxiety, nausea and vomiting during the recovery phase of anesthesia [Padfield NL, Int rduction, history and development, In: Padfield NL (Ed.) Ed., Total Intravenous Anesthesia, Butterworth Heinem...

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): C07F9/12C07F9/09C07C229/08A61K31/661A61K31/225A61P23/00
Inventor 杨成
Owner HC SYNTHETIC PHARMA CO LTD
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