Method for preparing metroprolol succinate conforming to European pharmacopoeia and United States pharmacopeia

A technology of metoprolol succinate and US Pharmacopoeia, applied in the field of drug synthesis, can solve problems such as unfavorable commercial production, inability to effectively reduce residual isopropylamine, potential safety hazards, etc., achieves benefits such as commercial production, reduction of post-processing steps, and savings The effect of production costs

Inactive Publication Date: 2017-06-20
上海华源医药科技发展有限公司
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  • Abstract
  • Description
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  • Application Information

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Problems solved by technology

Therefore, the main deficiency of the synthetic route provided by patent US 3,873,600 and patent US 3,998,790 is: the residual isopropylamine cannot be effectively reduced to meet the requirements of the Pharmacopoeia; other deficiencies have: the diethyl ether with low boiling point and low flash point is used in the metoprolol extraction stage , has potential safety hazards to the human body and is not conducive to commercial production

Method used

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Examples

Experimental program
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Embodiment Construction

[0020] Test 1: Dissolve epoxide in isopropanol (1.0 volume), cool the solution to 10° C., slowly add 1.0 molar equivalent of isopropylamine, and keep the reaction at 30° C. for 24 hours. The TLC result was not in compliance with the specification.

[0021] Experiment 2: Dissolve epoxide in isopropanol (1.0 volume), cool the solution to 10° C., slowly add 2.0 molar equivalents of isopropylamine, and keep the reaction at 30° C. for 24 hours. The TLC result was not in compliance with the specification.

[0022] Experiment 3: Dissolve epoxide in isopropanol (1.0 volume), cool the solution to 10° C., slowly add 3.0 molar equivalents of isopropylamine, and keep the reaction at 30° C. for 24 hours. The TLC result was not in compliance with the specification.

[0023] Experiment 4: Dissolve epoxide in isopropanol (1.0 volume), cool the solution to 10° C., slowly add 4.4 molar equivalents of isopropylamine, and keep the reaction at 30° C. for 24 hours. TLC results meet the requireme...

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PUM

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Abstract

The invention discloses a method for preparing metroprolol succinate conforming to European pharmacopoeia and United States pharmacopeia. The method comprises the following steps of (1) determining an optimum molar ratio of epoxides and isopropamide through an orthogonal test; (2) carrying out reduced pressure distillation on a reactant so as to remove residual isopropamide as far as possible. According to the method provided by the invention, the residual isopropamide in metroprolol is reduced, a metroprolol succinate solution produced by utilizing the metroprolol synthesized by the method is clear, conforms to standards of European pharmacopoeia/British pharmacopoeia and United States pharmacopeia, and is high in product quality; a postprocessing step is reduced, and the usage of an extracting solvent is avoided, so that not only is the production cost reduced, but also the commercial production is facilitated.

Description

technical field [0001] The invention relates to a method for preparing metoprolol succinate monographs in compliance with the European Pharmacopoeia and the United States Pharmacopoeia, belongs to the field of drug synthesis, is an optimized synthesis process, and aims to improve the clarity of metoprolol succinate solution so that Meets the requirements of the European Pharmacopoeia / British Pharmacopoeia and the USP monographs. Background technique [0002] Metoprolol succinate is the succinate of metoprolol. According to literature reports, the main synthesis techniques of metoprolol are: ①.1,2-epoxy-3-p-[(β-methoxy base)-phenoxy group] propane (being called for short epoxide) and isopropylamine react in isopropanol, gained reactant is extracted with ether and dichloromethane, distills off extraction solvent and obtains metoprolol (patent US 3,873,600 and Patent US 3,998,790, patent US 3,998,790 is the same family patent as patent US 3,873,600, the original research paten...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C217/32C07C213/02C07C213/10
CPCC07C213/02C07C213/10C07C217/32
Inventor 徐艳梅郑云丽彭志红朱晓娟刘朝霞王进陈良强
Owner 上海华源医药科技发展有限公司
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