Pyrolytic diterpenoid alkaloid compound as well as preparation method and application thereof

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

Active Publication Date: 2020-07-24
CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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  • 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 does the structure of the toxic alkaloid transform during the sand-frying process? Is the toxicity of the transformed product reduced compared with the original alkaloid? And because the processing principle of the sand-frying method has not been clarified, the quality evaluation of the sand-stir-fried processed products is still judged by s

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  • Pyrolytic diterpenoid alkaloid compound as well as preparation method and application thereof
  • Pyrolytic diterpenoid alkaloid compound as well as preparation method and application thereof
  • Pyrolytic diterpenoid alkaloid compound as well as preparation method and application thereof

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Embodiment Construction

[0053] Raw material, equipment used in the specific embodiment of the present invention are all known products, obtain by purchasing commercially available products.

[0054] The preparation of embodiment 1 formula II compound

[0055] 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 column loading.

[0056] 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 (0.7L), 4:1:0.01 (0....

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Abstract

The invention provides a pyrolytic diterpenoid alkaloid compound shown as a formula I shown in the specification, or a salt, a stereoisomer or a solvate thereof, and a preparation method of the pyrolytic diterpenoid alkaloid compound. The invention also provides application of the compound or the salt thereof, the stereoisomer thereof or the solvate thereof in preparing medicines for preventing and/or treating ventricular premature beat, ventricular tachycardia and antiarrhythmia, and the clinical prospect is excellent.

Description

technical field [0001] The invention belongs to the field of medicine, in particular 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 more than 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; ③Patients with...

Claims

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Application Information

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IPC IPC(8): C07D209/56A61P9/06A61K31/403
CPCC07D209/56A61P9/06
Inventor 王毓杰王艳陶培康云雪孙海霞
Owner CHENGDU UNIV OF TRADITIONAL CHINESE MEDICINE
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