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Preparation method of betahistine

A betahistine and solvent technology, which is applied in the field of preparation of betahistine, can solve the problems of low conversion rate, large amount of methylamine salt, and long reaction time, and achieve the effect of short time and reducing the risk of solvent residue

Pending Publication Date: 2021-09-28
SHANGHAI ZHONGXI SUNVE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem to be solved by the present invention is to overcome the defects of long reaction time, low conversion rate, large amount of methylamine salt and many by-products in the existing preparation method of betahistine, and provide a double The preparation method of tahistine

Method used

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  • Preparation method of betahistine
  • Preparation method of betahistine

Examples

Experimental program
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Effect test

Embodiment 1

[0047]

[0048] In the microchannel reaction device, the diameter of the connecting pipe is 1.0mm, and the volume of the microchannel reactor is 2.5mL.

[0049] 1. Take 2-vinylpyridine (3.15g, 30mmol), add ethanol to dilute to 15mL; 2. Take methylamine hydrochloride (4.05g, 60mmol), add water to dilute to 15mL, and use this as reaction solution 1 and Reaction solution 2 is waiting to be fed. Adjust the back pressure valve to control the pressure of the reaction system to 1.0MPa, and connect a section of 2m long pre-cooling pipeline to the front end of the back pressure valve. The temperature heater is controlled to reach 170°C, and the two materials are pumped into the microchannel reactor through the mixer. The fluid of reaction solution 1 flows through the microreactor at 0.5 mL / min, and the fluid of reaction solution 2 flows through the microreactor at 0.5 mL / min. The molar ratio of 2-vinylpyridine to methylamine hydrochloride is 1:2, and the reaction residence time is...

Embodiment 2

[0051] In the microchannel reaction device, the diameter of the connecting pipe is 1.0mm, and the volume of the microchannel reactor is 2.5mL.

[0052] 1. Take 2-vinylpyridine (3.15g, 30mmol), add toluene to dilute to 15mL; 2. Take methylamine hydrochloride (4.05g, 60mmol), add water to dilute to 15mL, and use this as reaction solution 1 and Reaction solution 2 is waiting to be fed. Adjust the back pressure valve to control the pressure of the reaction system to 1.0MPa, and connect a section of 2m long pre-cooling pipeline to the front end of the back pressure valve. The temperature heater is controlled to reach 170°C, and the two materials are pumped into the microchannel reactor through the mixer. The fluid of reaction solution 1 flows through the microreactor at 0.5 mL / min, and the fluid of reaction solution 2 flows through the microreactor at 0.5 mL / min. The molar ratio of 2-vinylpyridine to methylamine hydrochloride is 1:2, and the reaction residence time is 2.5min. The...

Embodiment 3

[0054]

[0055] In the microchannel reaction device, the diameter of the connecting pipe is 1.0mm, and the volume of the microchannel reactor is 2.5mL.

[0056] 1. Take 2-vinylpyridine (3.15g, 30mmol), add toluene and dilute to 15mL; 2. Take methylamine sulfate (4.81g, 30mmol), add water and dilute to 15mL, and use them as reaction solution 1 and reaction Liquid 2 awaits feed. Adjust the back pressure valve to control the pressure of the reaction system to 1.0MPa, and connect a section of 2m long pre-cooling pipeline to the front end of the back pressure valve. The temperature heater is controlled to reach 170°C, and the two materials are pumped into the microchannel reactor through the mixer. The fluid of reaction solution 1 flows through the microreactor at 0.5 mL / min, and the fluid of reaction solution 2 flows through the microreactor at 0.5 mL / min. The molar ratio of 2-vinylpyridine to methylamine hydrochloride is 1:1, and the reaction residence time is 2.5min. The co...

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Abstract

The invention discloses a preparation method of betahistine. The preparation method comprises the following steps: in a continuous flow reactor, 2-vinylpyridine and a methylamine salt aqueous solution are subjected to a reaction, and betahistine is obtained, wherein the 2-vinylpyridine is not diluted or is fed after being diluted by a solvent; the retention time of the reaction is not less than 0.6 min; the reaction temperature ranges from 100 DEG C to 250 DEG C. The betahistine prepared by the method has the advantages of high conversion rate of raw materials, high selectivity and yield of products, low solvent residue and short reaction time.

Description

technical field [0001] The invention relates to a preparation method of betahistine. Background technique [0002] Betahistine Hydrochloride (Betahistine Hydrochloride) chemical name is N-methyl-2-pyridylethylamine dihydrochloride, is a histamine H1 receptor agonist, clinically as a vasodilator, mainly used To treat various vertigo syndromes, chronic ischemic cerebrovascular diseases, Meniere's syndrome (an idiopathic inner ear disease) and related vertigo symptoms, etc. Betahistine hydrochloride is currently clinically used in the treatment of U.S. One of the most commonly prescribed medications for Neal's syndrome. It binds to vascular smooth muscle H1 receptors, can increase the blood flow of cardiovascular and cerebrovascular and peripheral blood vessels, improve microcirculation, and reduce the aggregation degree of red blood cells and platelet adhesion rate, thereby improving blood viscosity and hypercoagulation state. Increase the permeability of the capillary wall,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D213/38
CPCC07D213/38
Inventor 颜国明尹超俞伟叶金星孙茂林马跃跃程瑞华梁超茗付有天李杰
Owner SHANGHAI ZHONGXI SUNVE PHARMA
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