Method for preparing cilnidipine used as dihydropyridine calcium antagonist

A technology of cilnidipine and calcium antagonist, which is applied in the field of pharmaceutical preparation, can solve the problems of difficulty in obtaining intermediate 2, complex by-products of reaction products, and difficulty in industrialized production, etc., and achieves mild process conditions, simple post-processing, and reaction cycle. short effect

Inactive Publication Date: 2009-12-16
上海医药科技发展有限公司
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AI Technical Summary

Problems solved by technology

But this method is difficult to obtain purer intermediate 2 in the preparation process, and if the impurity that intermediate 2 exists directly reacts with 3 through separation, will bring complicated by-product to reaction product, to aftertreatment There are higher requirements, and generally all must be separated by column chromatography, so this method is difficult to carry out industrial production

Method used

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  • Method for preparing cilnidipine used as dihydropyridine calcium antagonist
  • Method for preparing cilnidipine used as dihydropyridine calcium antagonist
  • Method for preparing cilnidipine used as dihydropyridine calcium antagonist

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Embodiment 1

[0020] Preparation of Cinnamyl β-aminocrotonate (5)

[0021] Cinnamyl acetoacetate (100g, 0.458mol) was dissolved in absolute ethanol (50ml), cooled to 0-5°C under stirring, passed through ammonia gas for 3 hours, kept warm (0-5°C) for 6 hours, and vacuumed Unreacted ammonia gas was cooled overnight and filtered to obtain white crystal 5 with a weight of 78.6 g and a yield of 78.9%.

Embodiment 2

[0023] Preparation of Cinnamyl β-aminocrotonate (5)

[0024] Cinnamyl acetoacetate (100g, 0.458mol) was dissolved in anhydrous methanol (80ml), cooled to 0-5°C under stirring, passed through ammonia gas for 3 hours, kept warm (0-5°C) for 6 hours, and vacuumed Unreacted ammonia gas was cooled overnight and filtered to obtain white crystal 5 with a weight of 82.5 g and a yield of 82.8%.

Embodiment 3

[0026] Preparation of Cinnamyl β-aminocrotonate (5)

[0027] Cinnamyl acetoacetate (100g, 0.458mol) was dissolved in anhydrous n-propanol (45ml), cooled to 0-5°C under stirring, passed through ammonia gas for 3 hours, kept warm (0-5°C) for 6 hours, and depressurized The unreacted ammonia gas was pumped out, cooled overnight, and filtered to obtain white crystal 5 with a weight of 75.2 g and a yield of 75.5%.

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Abstract

The invention provides a method for preparing cilnidipine used as a dihydropyridine calcium antagonist, which comprises the following steps: 2-(3-nitrobenzyl) acetoacetic acid 2-methoxyethyl acetate 4 and beta-amino crotonic acid cinnamic ester 5 react in an alcohol solvent to obtain a coarse product of cilnidipine 1, and the coarse product of the cilnidipine 1 is recrystallized to obtain the cilnidipine 1. The method has the advantages of short reaction period, simple and convenient after-treatment, simple synthetic route, moderate process condition, and the like and is suitable for industrial production.

Description

technical field [0001] The present invention relates to medicine preparation. Specifically relates to a preparation method of dihydropyridine calcium antagonist cilnidipine. Background technique [0002] With the development of social economy and the improvement of people's living standards and the change of diet structure, cardiovascular disease has become one of the main diseases that affect the health of the broad masses of the people and hinder economic development, bringing great harm to society and families. stress and burden. According to the statistics of relevant departments, the prevalence of hypertension in the Chinese population is as high as 12%, and there is a gradual increase trend. If high blood pressure is not controlled, it may cause serious secondary diseases such as stroke and myocardial infarction, and make patients disabled and dead. In short, hypertension has become one of the main diseases that threaten human life. Therefore, the development of hy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90A61P9/12
Inventor 黄君勤初秀海傅自勤
Owner 上海医药科技发展有限公司
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