Double-effect anesthetic and preparation method and application thereof

A technology of drugs and compounds, applied in the field of medicine, can solve problems such as unpredictable drug interactions and complicated methods, and achieve the effects of strong intraoperative controllability, reduced incidence and severity, and quick recovery of patients.

Active Publication Date: 2016-07-13
GUANGDONG JIABO PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Such a method is complex, and possible

Method used

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  • Double-effect anesthetic and preparation method and application thereof
  • Double-effect anesthetic and preparation method and application thereof
  • Double-effect anesthetic and preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0033] Embodiment 1: Flurbiprofen reacts with propofol potassium salt to prepare compound of the present invention (1)

[0034] A) Preparation of propofol potassium salt: add 24.9g propofol (0.14mol), 8.4g potassium hydroxide (0.15mol) and 300mL toluene into a 500mL three-necked flask, stir, heat up to 100°C for reflux reaction for 3h , using a water separator to continuously separate the water produced by the reaction. Stop the reaction when no more water comes out of the trap. The system was transferred to a single-necked bottle and concentrated under reduced pressure to remove the solvent toluene to obtain a light yellow crude product of propofol potassium salt. The crude product was stirred with 150 mL butanone for 8 min, the insoluble matter was removed by filtration, and the filtrate was concentrated and dried under reduced pressure to obtain light yellow propofol potassium salt;

[0035] B) Dissolve the above propofol potassium salt with 300mL acetonitrile, transfer t...

Embodiment 2

[0036] Embodiment 2: Compound of the present invention (1) prepared by the reaction of flurbiprofen acyl chloride and propofol

[0037] A) Preparation of flurbiprofen acyl chloride: get 53.7g flurbiprofen (0.22mol) into a 500mL dry three-necked flask, add 150mL dichloromethane, stir, and control the temperature in an ice bath at 0-5°C, preferably 3 ℃, slowly add 49.3mL of thionyl chloride dropwise, slowly warm up to room temperature after dropping, stir and react for 4 hours, and perform TLC reaction. After the reaction is completed, excess thionyl chloride is recovered under reduced pressure to obtain a light yellow oil;

[0038] B) Take 39.2g of propofol (0.22mol), 50mL of pyridine and 100mL of dichloromethane into a 500mL dry there-necked flask, stir; control the temperature at 0-10°C, preferably 5°C, put the shallow The yellow oil was dissolved in 150mL of dichloromethane and slowly added dropwise to the system. After the drop was completed, the temperature was raised to r...

Embodiment 3

[0039]Embodiment 3: Compound of the present invention (1) prepared by reacting flurbiprofen acyl bromide and propofol sodium salt

[0040] A) Add 34.2g flurbiprofen (0.14mol) into a 250mL dry there-necked flask, add 120mL tetrahydrofuran; stir; control the temperature in an ice bath at 0-5°C, preferably 3°C, and slowly add 20mL of phosphorus oxybromide dropwise , slowly warming up to room temperature after dropping, stirring and reacting for 3h, carrying out TLC reaction, recovering excessive phosphorus oxybromide under reduced pressure after the completion of the reaction to obtain light yellow oil, dissolving the above light yellow oil in 100mL dichloromethane to obtain Dichloromethane solution containing acid bromide;

[0041] B) Add 24.9g of propofol (0.14mol), 3.6g of sodium hydride (0.15mol) and 300mL of tetrahydrofuran into a 500mL three-necked flask, and stir at room temperature for 4 hours; after the above system is concentrated and dried under reduced pressure, add 1...

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Abstract

The invention belongs to the technical field of medicine and particularly relates to a double-effect anesthetic and a preparation method and application thereof.The invention discloses a compound shown in the general formula (I).The compound can generate analgesic flurbiprofen and anesthetic propofol after hydrolysis, the analgesic and the tranquilizer are combined, dosage frequency of anesthetists is reduced, the anesthetic process is quicker, the occurrence rate and the severity of propofol injection pain can be remarkably reduced, adverse reactions of single drug are reduced, and the anesthetic has the advantages that the anesthetic takes effects quick, lasting time is short, anesthetic efficiency is high, controllability in operation is high, and patients recover quickly.Please see the structural formula in the description, wherein R refers to O or a radical group in the description, and n is 2-4.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a double-effect anesthetic and its preparation method and application. Background technique [0002] Propofol is an alkylphenol short-acting general intravenous anesthetic, which is commonly used clinically for the induction and maintenance of anesthesia and the sedation of critically ill patients in the ICU. It has the advantages of rapid effect, stable induction, strong controllability, short action time, rapid and stable recovery, and few side effects. Propofol has excellent properties and good application prospects, but because of its weak analgesic effect, injection pain is the most common adverse reaction of propofol emulsion. Literature reports [Wu Yin, Fourth Military Medical University, doctoral dissertation], the incidence of injection pain in adults is 28%-90%, while the incidence in children is 28-85%. Due to the high incidence of propofol injection pai...

Claims

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Application Information

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IPC IPC(8): C07C69/65C07C67/14A61K31/216C07C67/08A61P23/00
CPCC07C37/64C07C67/08C07C67/14C07C69/65C07C39/235
Inventor 徐礼锋曽少群李庆岳峰廖泳强
Owner GUANGDONG JIABO PHARM CO LTD
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