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A kind of pyrolysis type diterpene alkaloid compound and its preparation method and application

A technology for diterpene alkaloids and compounds, applied in the field of medicine, can solve the problems of arrhythmia, cardiotoxicity, lack of quantitative quality control indicators, etc.

Active Publication Date: 2022-05-03
CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the processing principle of the sand-frying method has not been fully elucidated. How to transform the structure of the toxic alkaloid during the sand-frying process, and whether the toxicity of the transformed product is lower than that of the prototype alkaloid, and because the processing principle of the sand-frying method has not yet been clarified, the sand-stirred cannon The quality evaluation of products is still judged by subjective experience such as: the medicinal materials are fried until "the outer skin is browned and the section is yellow", and there is a lack of quantitative quality control indicators.
In addition, studies have shown that although some diterpene alkaloids have similar structures, they have opposite effects. For example, some can cause arrhythmia and have cardiotoxicity, while others have the effect of treating arrhythmia.

Method used

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  • A kind of pyrolysis type diterpene alkaloid compound and its preparation method and application
  • A kind of pyrolysis type diterpene alkaloid compound and its preparation method and application
  • A kind of pyrolysis type diterpene alkaloid compound and its preparation method and application

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Embodiment Construction

[0054] The raw materials and equipment used in the specific embodiment of the present invention are all known products, obtained by purchasing commercially available products.

[0055] The preparation of embodiment 1 formula II compound

[0056] Take 500 mg of 3-acetylaconitine (3-acetylaconitine), put it in a 250ml round-bottomed flask, add an appropriate amount of dichloromethane to dissolve, and evaporate the solvent to dryness at 40°C with a rotary thin film evaporator to make 3-acetylaconitine evenly Adhere to the inner wall of the round bottom flask, and put it in an oil bath at 180°C for 15 minutes, take it out, and let it cool to obtain the processed product of 3-acetylaconitine (400 mg), which is used for loading on the column.

[0057] The processed product of 3-acetylaconitine was subjected to silica gel column chromatography (200-300 mesh, 120g) for separation and purification, respectively with petroleum ether-acetone-triethylamine (8:1:0.01 (0.63L), 6:1:0.01 (0....

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Abstract

The present invention provides a pyrolytic diterpene alkaloid compound represented by formula I, or a salt thereof, or a stereoisomer thereof, or a solvate thereof, and a preparation method thereof. The present invention also provides the application of the compound or its salt, or its stereoisomer, or its solvate in the preparation of prevention and / or treatment of ventricular premature beats, ventricular tachycardia, and antiarrhythmic drugs, and the clinical prospect excellent.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a pyrolysis type diterpene alkaloid compound and its preparation method and application. Background technique [0002] Arrhythmia is a clinically common and very dangerous cardiovascular disease. For a long time, people have been devoting themselves to the research of antiarrhythmic drugs, but there has been no obvious breakthrough in the past 20 years. [0003] Clinical treatment of arrhythmias can use antiarrhythmic drugs, or choose radiofrequency ablation and implantable automatic cardioverter defibrillator (ICD). [0004] Antiarrhythmic drugs still play an important role in the treatment of arrhythmias for the following reasons: (1) Most tachyarrhythmias require drugs to terminate the attack during acute attacks; (2) Some supraventricular premature beats and premature ventricular beats that cause symptoms need to be controlled with drugs and prevention of recurrence; ③Pa...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D221/22A61P9/06
CPCC07D221/22A61P9/06A61K31/439
Inventor 王毓杰王艳陶培康云雪孙海霞
Owner CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE