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Propofol compound as well as preparation method and application thereof

A technology of propofol and compound, applied in the field of propofol compound and preparation thereof, can solve the problems of poor antioxidant performance, influence on clinical use effect, poor water solubility of propofol and the like

Pending Publication Date: 2022-03-01
深圳市爱卫德为生物科技有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of this application is to provide a kind of propofol and its preparation method, aiming at solving the problem that the existing propofol has poor water solubility and poor anti-oxidation performance, which affects the clinical use effect

Method used

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  • Propofol compound as well as preparation method and application thereof
  • Propofol compound as well as preparation method and application thereof
  • Propofol compound as well as preparation method and application thereof

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preparation example Construction

[0037] The second aspect of the embodiment of the present application provides a preparation method of a propofol compound, the preparation method comprising the following steps:

[0038] S10: providing the reactant shown in formula I, propofol shown in formula II, and salvianolic acid A shown in formula III;

[0039] S20: dissolving the reactant and propofol in a first solvent, and performing a first coupling reaction under the conditions of a first coupling agent to generate a first intermediate product as shown in formula IV;

[0040] S30: removing the protecting group contained in the first intermediate product to obtain a second intermediate product as shown in formula V;

[0041] S40: Mix the second intermediate product with the salvianolic acid A, and perform a second coupling reaction under the conditions of the second coupling agent to generate salvianolic acid A-propofol as shown in formula VI compound;

[0042]Wherein, the R groups in the formulas I, IV, V and VI ...

Embodiment 1

[0068] The present embodiment provides a kind of preparation method of propofol compound, comprises the following steps:

[0069] S1: Provide 2-(tert-butylcarbonylamino)acetic acid, propofol, and salvianolic acid A with the R group being H as the reaction raw materials;

[0070] S2: 4.29g, 24.5mmol of 2-(tert-butylcarbonylamino)acetic acid and 3.3g, 18.5mmol of propofol were dissolved in dichloromethane, and 3.15g, 16.5mmol of propofol were added under nitrogen atmosphere EDC hydrochloride and 0.52g, 4.3mmol of DMAP, the resulting reaction mixture was stirred overnight at a temperature of 0-37°C, then the reaction mixture was washed with water twice, and dried with a desiccant containing magnesium sulfate; after solvent evaporation, Using hexane solvent column chromatography containing 1%-10% ethyl acetate to obtain yellow liquid 2,6-diisopropylphenyl 2-(tert-butylcarbonylamino) acetate (the first intermediate product) . Its reaction equation is as follows:

[0071]

[0...

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Abstract

The invention relates to the technical field of biological medicine, and provides a propofol compound, the molecular structural formula of the propofol compound is as shown in the following structural general formula: R group in the structural general formula is H or a variable group of amino acid. According to the propofol compound provided by the invention, the propofol is modified by a salvianolic acid A group, so that the propofol compound provided by the invention has relatively high oxidation resistance and water solubility. After the propofol-salvianolic acid compound is injected into a body, peptide bonds (-CO-NH-) contained in the propofol-salvianolic acid compound can be quickly decomposed and released to obtain propofol and salvianolic acid A, and the calming and anesthetic efficacy of propofol is fully exerted; in addition, the propofol compound has water solubility, so that a lipid emulsion does not need to be additionally added as a solvent, and allergic reaction caused by allergy of a patient to lipids or proteins in the emulsion is avoided.

Description

technical field [0001] The application belongs to the technical field of biomedicine, and in particular relates to a propofol compound and its preparation method and application. Background technique [0002] Propofol, alias propofol or dipropofol, chemical name is 2,6-diisopropylphenol, molecular formula is C 12 h 18 O, the structural formula is as follows: [0003] [0004] It is a sedative anesthetic mainly used for the induction and maintenance of general anesthesia. [0005] Since propofol is soluble in most organic solvents and insoluble in water, all existing medicines use lipid emulsions as solvents. When propofol is used clinically, patients are prone to be allergic to the lipid or protein components in the emulsion. Reaction; During the intravenous injection, the patient experienced obvious local pain at the injection site. Studies have shown that the incidence of propofol intravenous pain is 28% to 90% in adults, and 28% to 85% in children. This pain can oc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C235/34C07C231/02A61K31/216A61K31/223A61P23/00
CPCC07C235/34A61P23/00Y02P20/55
Inventor 夏正远刘卫徐爱民刘丹勇
Owner 深圳市爱卫德为生物科技有限公司
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