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Preparation method of orthographic optimizing betahistine hydrochloride

A technology of betahistine and hydrochloric acid, which is applied in the field of drug preparation, can solve the problems of long reaction time and low reaction yield, and achieve the effects of reduced production cost, simple process flow and mild reaction

Inactive Publication Date: 2018-03-23
SHAANXI QIYUAN TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current method takes a long time to react and the reaction yield is low.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] The preparation method of orthogonal optimization betahistine hydrochloride of the present invention comprises the following steps:

[0015] The first step, the preparation of 2-hydroxyethylpyridine, according to 2-picoline:paraformaldehyde feed ratio 1:0.57 (molar ratio), raw material is added in the reaction bottle, fill with nitrogen, stir 20h, stirring temperature is 125°C and a pressure of 4 atmospheres, then distilled under reduced pressure, collecting fractions at a temperature of 130-145°C and a pressure of 16 mm Hg to obtain light yellow oily 2-hydroxyethylpyridine;

[0016] The second step, the preparation of 2-vinylpyridine, add 2-hydroxyethylpyridine to the three-necked flask, according to the ratio of 2-hydroxyethylpyridine: sodium hydroxide 1:0.05, after adding sodium hydroxide, heat to 95-100 degrees, after stirring for 2 hours, the water layer was separated, the oil layer was distilled under reduced pressure, and the temperature was 65-70 degrees, and th...

Embodiment 2

[0020] The preparation method of orthogonal optimization betahistine hydrochloride of the present invention comprises the following steps:

[0021] The first step, the preparation of 2-hydroxyethylpyridine, according to 2-picoline:paraformaldehyde feed ratio 1:0.57 (molar ratio), raw material is added in the reaction bottle, fill with nitrogen, stir 20h, stirring temperature is 125°C and a pressure of 4 atmospheres, then distilled under reduced pressure, collecting fractions at a temperature of 130-145°C and a pressure of 16 mm Hg to obtain light yellow oily 2-hydroxyethylpyridine;

[0022] The second step, the preparation of 2-vinylpyridine, add 2-hydroxyethylpyridine to the three-necked flask, according to the ratio of 2-hydroxyethylpyridine: sodium hydroxide 1:0.05, after adding sodium hydroxide, heat to 95-100 degrees, after stirring for 2 hours, the water layer was separated, the oil layer was distilled under reduced pressure, and the temperature was 65-70 degrees, and th...

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PUM

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Abstract

The invention discloses a preparation method of orthographic optimizing betahistine hydrochloride, and relates to the field of drug preparation. The preparation method includes the steps: adding raw materials into a reaction bottle according to the feeding ratio (molar ratio) of 2-methylpyridine to paraformaldehyde of 1:0.57, leading in nitrogen, stirring mixture for 20 hours at the temperature of125 DEG C and at 4 barometric pressure, performing reduced pressure distillation, and collecting distillation cut at the temperature of 130-145 DEG C and under the pressure of 16mm mercury columns toobtain light-yellow oily 2-hydroxyethyl pyridine; adding the 2-hydroxyethyl pyridine into a three-opening bottle, adding sodium hydroxide according to the feeding ratio of 2-(2-Hydroxyethyl)pyridineto sodium hydroxide of 1:0.05, heating the mixture to reach 95-100 DEG C, stirring the mixture for 2 hours, removing a water layer, performing reduced pressure distillation on an oil layer, and collecting the distillation cut at the temperature of 65-70 DEG C and under the pressure of 17mm mercury columns to obtain 2-vinylpyridine. The preparation method is simple in technological process, safe tooperate and mild in reaction, production efficiency and product quality can be greatly improved, and production cost is reduced.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to an orthogonally optimized preparation method of betahistine hydrochloride. Background technique [0002] The chemical name of betahistine hydrochloride is N-methyl-2-pyridylethylamine dihydrochloride. Receptor agonist, acting on vascular smooth muscle receptors, clinically used as a vasodilator, can increase the blood flow of the heart, cerebrovascular and peripheral blood vessels, improve microcirculation, and reduce the aggregation of red blood cells and the adhesion rate of platelets. Through the improvement of blood circulation, the blood viscosity and hypercoagulation state can be alleviated, the permeability of capillary wall can be increased, and the reverse absorption of extracellular fluid can be promoted, so as to reduce the viscosity of blood, and it can be used to treat coronary insufficiency. , Ischemic cerebrovascular diseases such as cerebral thrombosis, cerebr...

Claims

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Application Information

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IPC IPC(8): C07D213/38
CPCC07D213/38
Inventor 张淑芬
Owner SHAANXI QIYUAN TECH DEV
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