- Synthesis method of itopride hydrochloride
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The invention discloses a synthesis method of itopride hydrochloride, and relates to the technical field of organic synthesis. Hydroxybenzylamine is taken as starting material, in non-polar solvent, in the presence of an acid-binding agent, the Hydroxybenzylamine and 3,4-dimethoxybenzoyl chloride are subjected to amidation to obtain an intermediate N-(4-hydroxyl) benzyl-3,4-dimenthoxybenzamide, and in polar solvent, in the presence of a catalyst, the intermediate N-(4-hydroxyl) benzyl-3,4-dimenthoxybenzamide and 2-chlorine-N,N-dimethylethylamine are subjected to etherification to obtain the itopride hydrochloride. According to the method, the raw materials are easy to obtain, the route is short, only two steps of synthetic reactions are needed, the high yield of 85-97% can be achieved in each step, by means of amidation and etherification with high product purity, a dangerous process of high-pressure hydrogenation is avoided successfully, and meanwhile, the production and raw materialcosts are greatly reduced.
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Paragraph 0022-0025
(2018/04/21)
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- Preparation method of medicine of itopride hydrochloride for promoting gastrointestinal motility
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The invention discloses a preparation method of medicine of itopride hydrochloride for promoting gastrointestinal motility. The method comprises the following steps that p-hydroxy methylbenzene is used as a raw material to take a reaction with dimethylaminoethyl chloride hydrochloride; then, 4-(2-dimethylamino oxethyl) benzyl bromide is synthesized through bromination; next, the 4-(2-dimethylamino oxethyl) benzyl bromide and 3,4-dimethoxybenzonitrile take a reaction to obtain a product of itopride under the solvent-free condition through copper trifluoromethanesulfonate catalysis. The preparation method has the advantages a bran-new synthesis route is provided; the itopride is synthesized through Ritter reaction under the solvent-free condition; the advantage of green and environment-friendly effects is realized; meanwhile, the used raw material resources are wide and sufficient; the price is low; the reaction conditions are mild.
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- Itopride preparation method
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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.
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- Preparation method of itopride hydrochloride
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The invention relates to a preparation method of itopride hydrochloride. The preparation method includes: using 2-dimethylaminoethyl chloride hydrochloride and phenol as starting materials for reaction; subjecting the starting materials to etherification, chloromethylation, amino substitution, amidation and salifying to obtain itopride hydrochloride. Chloromethylation promoted by C/CHO is adopted, so that a step of imine reduction is omitted, solid residue generated by a reductant is eliminated, and reaction safety is improved; raw materials used in the method are low in price, sufficient in market supply and easy to purchase; reaction in each step is classic, and the preparation method is safe, easy to control and suitable for industrial production.
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- Novel method for preparing itopride and the intermediate obtained from the method
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As well as novel intermediates of norcisapride is lengthwisely the present invention refers to and is lengthwisely of formula iii. using the same and manufacturing method relates to manufacturing method. By of the present invention manufacturing method, benzamide derivatives via a stable final is lengthwisely norcisapride high purity and high yield, widely used as an, of the present invention manufacturing method flat plate is transferred to print the can be produced at low cost, is lengthwisely of formula iii. for mass production and available.
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- NOVEL PROCESS FOR SYNTHESIS OF ITOPRIDE AND ITS NOVEL INTERMEDIATE N-(4-HYDROXYBENZYL)- 3,4-DIMETHOXYBENZAMIDE
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The present invention relates to a novel and improved process for the preparation of N-[4-[2-(dimethylamino)ethoxy]benzyl]-3,4-dimethoxybenzamide—known as Itopride, via a novel intermediate N-(4?hydroxybenzyl)-3,4-dimethoxybenzamide.
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Page/Page column 4
(2009/07/18)
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- A NOVEL PROCESS FOR SYNTHESIS OF ITOPRIDE AND IT’S NOVEL INTERMEDIATE-N-(4-HYDROXYBENZYL)-3,4-DIMETHOXYBENZAMIDE
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The present invention relates to a novel and improved process for the preparation of N-[4-[2-(dimethylamino)ethoxy]benzyl]-3,4-dimethoxybenzamide-known as Itopride, via a novel intermediate N-(4~hydroxybenzyl)-3,4-dimethoxybenzamide.
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Page/Page column 11
(2008/06/13)
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- PROCESS FOR PREPARING ITOPRIDE HYDROCHLORIDE
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Process for preparing itopride hydrochloride comprising: a) Reacting 4-hydroxybenzaldehyde with 2-dimethylaminoethyl chloride in the 5 presence of a weak inorganic base to obtain 4-(2-dimethylaminoethoxy)- benzaldehyde, b) Reacting 4-(2-dimethylaminoethoxy)-benzaldehyde with hydroxylamine hydrochloride in an acid environment to obtain 4-(2-dimethylaminoethoxy)- benzaldoxime hydrochloride, 10 c) Reacting of 4-(2-dimethylaminoethoxy)-benzaldoxime hydrochloride in the presence a reducing agent to 4-(2-dimethylaminoethoxy)-benzylamine, d) Reacting 4-(2-dimethylaminoethoxy)-benzylamine with veratric acid chloride in the presence of a tertiary amine to obtain itopride, e) Salifying itopride with hydrochloric acid to obtain itopride hydrochloride, 15 characterized in that the reducing agent employed in step (c) is powdered zinc.
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Page/Page column 7
(2010/11/30)
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- Amide compounds, process for preparing the same, and composition for activating gastric motor function containing the same
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Amide-compounds represented by the formula (I): STR1 wherein R1 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino which can be substituted by lower alkyl, nitro, cyano, sulfamoyl which can be substituted by lower alkyl, R2 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino, nitro, wherein R1 and R2 can be combined to form methylenedioxy, R3 means hydrogen, lower alkyl, halogen, or amino, R4 and R5 may be the same or different and each represents lower alkyl or wherein R4 and R5 may be combined together with nitrogen to form 1-pyrrolidinyl or piperidino, and pharmacologically-acceptable acid-addition salts thereof, which exhibit excellent effects in the activation of gastric motor function, a process for preparation pharmaceutical compositons thereof, as well as a method for the treatment of a subject suffering from an ailment associated with inadequate gastric motor function by administrating such a compound to the said subject, are all disclosed.
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