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Synthesis method of metoprolol succinate

A technology for the synthesis of metoprolol succinate, which is applied in the field of medicinal chemistry, can solve the problems of low yield of synthetic routes, environmental pollution, etc., and achieve the effects of simple operation, environmental friendliness and good quality

Inactive Publication Date: 2013-05-15
北京华素制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The yields of the traditional synthetic routes of metoprolol are all low, and there is certain pollution to the environment

Method used

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  • Synthesis method of metoprolol succinate
  • Synthesis method of metoprolol succinate

Examples

Experimental program
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Embodiment 1

[0052] A. Preparation of 3-[4-(2-methoxyethyl)phenoxy]-1,2-propylene oxide (compound M1)

preparation example A-1

[0054] Put 40L of purified water and 2.31Kg of sodium hydroxide into a 100L glass reactor, and stir until the solids are fully dissolved. Weigh 8Kg of 4-(2-methoxyethyl)phenol, add it into a glass reactor, and stir for 30 minutes. Measure 4.86Kg of epichlorohydrin, add it into a glass reactor, heat and stir for 10 hours, and control the internal temperature at 30°C. After the reaction was completed, the heating was stopped, and 16 L of ethyl acetate was added to the glass reactor for extraction. The organic phase was dried over anhydrous magnesium sulfate. Filter and distill the filtrate under reduced pressure with a rotary evaporator. 10.27Kg of 3-[4-(2-methoxyethyl)phenoxy]-1,2-propylene oxide (M1) was obtained with a yield of 93.8%.

preparation example A-2

[0056] Put 40L of purified water and 2.31Kg of sodium hydroxide into a 100L glass reactor, and stir until the solids are fully dissolved. Weigh 8Kg of 4-(2-methoxyethyl)phenol, add it into a glass reactor, and stir for 30 minutes. Measure 5.35Kg of epichlorohydrin, put it into a glass reactor, heat and stir for 6 hours, and control the internal temperature at 40°C. After the reaction was completed, the heating was stopped, and 16 L of ethyl acetate was added to the glass reactor for extraction. The organic phase was dried over anhydrous magnesium sulfate. Filter and distill the filtrate under reduced pressure with a rotary evaporator. 10.42Kg of 3-[4-(2-methoxyethyl)phenoxy]-1,2-propylene oxide (M1) was obtained with a yield of 95.2%.

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Abstract

The invention discloses a synthesis method of metoprolol succinate. The method mainly consists of the steps of: 1) taking 4-(2-methoxyethyl)phenol as a starting raw material, and letting it and epichlorohydrin to undergo a phenol etherification reaction; 2) subjecting the phenol etherification product and isopropylamine to an amination reaction so as to obtain metoprolol; and 3) making the metoprolol and succinic acid to form a salt, thus obtaining the metoprolol succinate. The synthesis method provided in the invention has the advantages of cheap and easily available raw materials and simple operation, thus being suitable for industrialized production.

Description

technical field [0001] The invention belongs to the technical field of medicinal chemistry, and more specifically relates to a synthetic method of metoprolol succinate. Background technique [0002] Metoprolol is a selective β1 receptor blocker and is one of the commonly used drugs for the treatment of hypertension, coronary heart disease, chronic heart failure and arrhythmia. Metoprolol belongs to class 2A, β1-blockers without partial agonistic activity (cardioselective β-blockers). It has selective blocking effect on β1-receptor, no PAA (partial agonistic activity), no membrane stabilizing effect. Metoprolol has no β-receptor agonism and almost no membrane activation. Beta-blockers have negative inotropic and chronotropic effects. Treatment with metoprolol attenuates the effects of catecholamines associated with physical and psychological stress, reducing heart rate, cardiac output, and blood pressure. Under stress, adrenaline secreted by the adrenal glands increases, ...

Claims

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Application Information

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IPC IPC(8): C07C217/32C07C213/04
Inventor 米春来陈凯魏淑冬边玢姚文静龙永鹏
Owner 北京华素制药股份有限公司
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