一种伊托必利的制备方法

Itopride preparation method

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.
本发明公开了一种伊托必利的制备方法,具体步骤如下:步骤一,2‑(二甲氨基)氯乙烷盐酸盐与对羟基苯甲醛合成4‑(2‑二甲氨基乙氧基)苯甲醛,然后在醇溶剂中还原合成4‑(2‑二甲氨基乙氧基)苄醇;步骤二,3,4‑二甲氧基苯甲醛与盐酸羟胺在醇溶剂中反应,然后在非极性溶剂中利用脱水剂脱水合成3,4‑二甲氧基苯甲腈;步骤三,4‑(2‑二甲氨基乙氧基)苄醇与3,4‑二甲氧基苯甲腈一步合成伊托必利;步骤四,将伊托必利溶于氯化氢的醇溶液中成盐得到盐酸伊托必利。本发明采用的原料来源广泛,制备工艺简单,适用于大规模的工业化生产;本发明的制备工艺没有危险工艺,生产设备简单,合成路线比现有的路线短,制备时间短,使用效果好。

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