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Itopride preparation method

A technology of itopride hydrochloride and dimethylaminoethoxy, which is applied in the field of preparation of itopride, can solve the problems of inconvenience for manufacturers, poor selectivity, and long routes, and achieve simple production equipment, short synthesis routes, Effects from a wide range of sources

Inactive Publication Date: 2017-03-22
安徽省诚联医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The synthetic route of existing itopride hydrochloride mainly contains following two kinds: a kind of scheme is that benzoyl chloride and amide react first, then etherification, but this method yield is lower, and selectivity is poor
Such as patent US2009177008, WO200774386; Another method is to etherify first, then synthesize benzylamine, and finally react with benzoyl chloride. This method is currently the main method for preparation, but the route is longer and the yield is lower. Such as patent WO2006051079, CN1706815, CN201210549091.5, all of which have brought inconvenience to the manufacturer

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] A kind of preparation method of itopride, concrete steps are as follows:

[0016] Step 1, take 80 g of p-hydroxybenzaldehyde, 128 g of potassium carbonate, 150 mL of DMF and 10 mL of isopropyl ether and stir, then add 101 g of 2-(dimethylamino) ethyl chloride hydrochloride to dissolve in DMF, and add 80 g of triethylamine solution, stirred and reacted at 80°C for 2h, cooled the reaction solution to room temperature, poured it into 700mL water, added 500mL chloroform for extraction, added 2 mol L-1 sulfuric acid 300mL to chloroform for extraction, and cooled the reaction solution to a mass fraction of 20 % sodium hydroxide solution 200mL was added to the water phase, then extracted with 1000mL ethyl acetate, dried with anhydrous sodium sulfate, recovered ethyl acetate under reduced pressure and distilled under reduced pressure, collected bp142-144℃ / 0.533kPa fraction, 110.2 g of 4-(2-dimethylaminoethoxy) benzaldehyde was obtained, and the yield reached 86.3%. 100 g of 4-(...

Embodiment 2

[0021] A kind of preparation method of itopride, concrete steps are as follows:

[0022] Step 1, take 160 g of p-hydroxybenzaldehyde, 101 g of potassium hydroxide, 200 mL of DMF and 20 mL of isopropyl ether and stir, then add 202 g of 2-(dimethylamino) ethyl chloride hydrochloride to dissolve in DMF, add triethyl A solution of 156 g of amine was stirred and reacted at 80 °C for 2 h, the reaction solution was cooled to room temperature, poured into 100 mL of water, extracted with 800 mL of chloroform, added 800 mL of 2 mol L-1 sulfuric acid to the chloroform for extraction, and the mass fraction was calculated under ice water cooling Add 200mL of 20% sodium hydroxide solution into the water phase, extract with 1000mL of ethyl acetate, dry over anhydrous sodium sulfate, recover ethyl acetate under reduced pressure and distill under reduced pressure, collect bp142-144 ℃ / 0.533 kPa fraction , 216.2 g of 4-(2-dimethylaminoethoxy) benzaldehyde was obtained, and the yield was 84.7 %; ...

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PUM

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Abstract

The invention discloses an itopride preparation method, the method comprises the steps of 1, 2-(dimethylamino) chloroethane hydrochloride and hydroxybenzaldehyde synthesizing into 4-(2- dimethylamino ethoxy) benzaldehyde, then synthesizing into 4-(2- dimethylamino ethoxy) benzyl alcohol in alcohol solvent by revivification; 2, in alcohol solvent 3, 4-dimethoxy benzaldehyde and hydroxylamine hydrochloride creating reaction, then in nonpolar solvent synthesizing into 3, 4- dimethoxybenzonitrile by dehydration using the dehydrant; 3, the 4-(2-dimethylamino ethoxy) benzyl alcohol and the 3, 4- dimethoxybenzonitrile synthesizing into itopride in one step; 4, obtaining hydrochloric acid itopride by dissolving itopride in hydrogen chloride alcohol solution and salifying. The adopted raw material in the method is wide in sourcing scope, simple in preparation processing, and is suitable for large scale industrialization production; the preparation process involves no danger process, the production equipment is simple, the synthesized circuit is shorter than the existed circuits, the preparation time is short and the use effect is good.

Description

technical field [0001] The invention relates to the field of medicine production, in particular to a preparation method of itopride. Background technique [0002] With the acceleration of the pace of life, the emergence of various environmental problems and the aggravation of food safety, people are more and more endangered by diseases, and people will use drugs to treat them when they are sick. Drugs refer to chemical substances that can affect the physiological, biochemical and pathological processes of the body, and are used for the prevention, diagnosis, treatment of diseases and family planning. Medicines include hypnotics, cold medicines, antipyretics, stomach medicines, and laxatives that are good for health. Itopride hydrochloride is a new type of gastrointestinal motility drug developed by Japan Hokuriku Pharmaceutical Co., Ltd. It exerts its curative effect by antagonizing dopamine D2 receptors and anticholinease, and is suitable for various diseases caused by fun...

Claims

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Application Information

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IPC IPC(8): C07C231/06C07C235/48C07C253/00C07C255/54C07C213/08C07C217/20C07C213/06C07C217/22C07C231/12
CPCC07C231/06C07C213/06C07C213/08C07C231/12C07C253/00
Inventor 刘辉
Owner 安徽省诚联医药科技有限公司
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