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Method for synthesizing phthaloyl amlodipine

A technology of phthaloyl ammonium chloride and phthalimide ethoxy, which is applied in the field of drug synthesis, can solve the problems of delayed drug action, slow binding and dissociation speed, etc., and achieve excellent quality, Fully responsive and easy to operate

Inactive Publication Date: 2017-05-31
千辉药业(安徽)有限责任公司
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  • Abstract
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Problems solved by technology

[0003] It is characterized by slow binding and dissociation with receptors, so the drug effect appears later and lasts longer

Method used

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  • Method for synthesizing phthaloyl amlodipine
  • Method for synthesizing phthaloyl amlodipine
  • Method for synthesizing phthaloyl amlodipine

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Embodiment Construction

[0026] The technical solutions of the present invention will be further described below in conjunction with specific examples, and the examples should not be construed as limitations on the technical solutions.

[0027] A kind of synthetic method of phthaloyl amlodipine, comprises the following steps:

[0028] (1) Synthesis of N-hydroxyethylphthalimide

[0029]

[0030] Add 200g of phthalic anhydride and 600ml of toluene to the reaction flask equipped with a water separator, raise the temperature, add 100g of ethanolamine dropwise, reflux until the reaction is complete, cool and filter, dry at 80-90°C to obtain 247.6g of N-hydroxyethyl o-phthalate Dicarboximide, the yield is 96%.

[0031] (2) Synthesis of ethyl-4-(2-phthalimidoethoxy) ethyl acetoacetate

[0032]

[0033] a. Put 2400ml tetrahydrofuran into the reaction bottle A, stir and cool to below -10°C, add 750g N-hydroxyethylphthalimide and 345g NaH in turn (while cooling, stir at a low speed, N-hydroxyethylphthal...

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Abstract

The invention relates to the field of drug synthesis, particularly to a method for synthesizing phthaloyl amlodipine. The method for synthesizing the phthaloyl amlodipine comprises the following steps: (1) synthesis of N-hydroxyethyl phthalimide; (2) synthesis of ethyl-4-(2-phthaloyl ethoxy) ethyl acetoacetate, wherein the ethyl-4-(2-phthaloyl ethoxy) ethyl acetoacetate is prepared by enabling the N-hydroxyethyl phthalimide to react with 4-chloroacetoacetate under a certain condition; (3) synthesis of phthaloyl amlodipine, wherein a target product is obtained by adding 2-chlorobenzaldehyde, acetic acid, piperidine and beta-methyl aminocrotonate to the ethyl-4-(2-phthaloyl ethoxy) ethyl acetoacetate in sequence under a certain condition to react with the ethyl-4-(2-phthaloyl ethoxy) ethyl acetoacetate, adding acetic acid to a reaction product after the reaction, and crystallizing, filtering, washing and drying the reaction product and the acetic acid. The method for synthesizing the phthaloyl amlodipine, provided by the invention, is efficient and easy to operate and can prepare the phthaloyl amlodipine with high yield and excellent quality.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to a synthesis method of phthaloyl amlodipine. Background technique [0002] Amlodipine, the chemical name is 3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(-2-chlorophenyl)-6-methyl-1,4- Dihydro-3,5-pyridinedicarboxylate is a dihydropyridine calcium ion antagonist developed by Pfizer in the 1990s. It is mainly used for the treatment of hypertension and angina pectoris as the first choice drug for the treatment of hypertension. , the sales volume ranks first in the world of cardiovascular drugs. [0003] It is characterized by slow binding and dissociation with receptors, so the drug effect appears later and lasts for a long time. The selective effect on vascular smooth muscle is greater than that of nifedipine. In patients with myocardial ischemia, this product can increase cardiac output and coronary flow, increase myocardial oxygen supply and reduce oxygen consumption, and improve e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
CPCC07D401/12
Inventor 杨会来毛杰孙学喜
Owner 千辉药业(安徽)有限责任公司
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