A kind of preparation method of nisoldipine impurity

A nisoldipine and impurity technology, which is applied in the field of preparation of nisoldipine impurities, can solve the problems of no drug efficacy and toxicity of the product, poor stability of nisoldipine, etc., and achieve the effects of high yield, low production cost, and simple processing method
CN112979538BActive Publication Date: 2022-03-08SOUTHEAST UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SOUTHEAST UNIV
Publication Date
2022-03-08

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Abstract

The invention discloses a preparation method of nisoldipine impurity. The nisoldipine impurity is 2,6-dimethyl-4-(2-nitrosophenyl)-1,4-dihydro-3,5-pyridinedicarboxylate methyl isobutyl ester, the structure is as follows: Ⅰ) as shown. The preparation method of the nisoldipine impurity is prepared by taking nisoldipine as a raw material, adding a free radical initiator, and undergoing one-step photodegradation. The method adopted in the present invention is simple, easy to operate, mild in reaction conditions, and simple in post-treatment process, and provides a new way for further identifying, separating, preparing and characterizing the nisoldipine impurities, improving the quality control level and medication safety of nisoldipine, It is beneficial to the control of the quality of medicines in the production process.
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Description

technical field

[0001] The invention relates to a preparation method of nisoldipine impurities, belonging to the technical field of drug synthesis. Background technique

[0002] Nisoldipine, yellow crystalline powder, chemical name: 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylic acid methyl ester iso Butyl ester, molecular formula C 20 h 24 N 2 o 6 , molecular weight 388.41.

[0003] Nisoldipine is currently the long-acting dihydropyridine calcium antagonist with the strongest selective vasodilation effect. It has significant medicinal effect on preventing coronary heart disease, hypertension and chronic congestive heart failure, and can reduce the risk of fatal ventricular fibrillation caused by acute myocardial infarction. Pharmacokinetic studies of different animals have shown that it is absorbed quickly and completely in the body, and has the longest duration. The plasma elimination half-life is as long as 42 to 54 hours. Effective drug in typ...

Claims

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