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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
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  • 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

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  • 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.

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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

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Application Information

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IPC IPC(8): C07F9/12C07F9/09C07C229/08A61K31/661A61K31/225A61P23/00
Inventor 杨成
Owner HC SYNTHETIC PHARMA CO LTD
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