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Prepn process of alizapride hydrochloride

A technology of hydrochloride and sodium nitrobenzoate is applied in the field of preparation of alipride hydrochloride to achieve the effect of reducing the amount of three wastes treated

Inactive Publication Date: 2007-11-07
苏州摩尔医药有限公司
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  • Abstract
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  • Claims
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Problems solved by technology

[0008] The technical problem to be solved by the present invention is to overcome the defects of the existing technology and provide a preparation method of aripride hydrochloride, which has the advantages of high yield, easy operation and less pollution

Method used

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Embodiment 1

[0030] 1. Preparation of intermediate 2-methoxy-4-amino-5-nitrobenzoic acid:

[0031] In the reaction flask, add 31.5 grams of 4-aminosalicylic acid and 80 ml of glacial acetic acid, add 20 grams of dimethyl carbonate under stirring, heat up and reflux for 4-10 hours, then add 60 grams of acid anhydride after cooling, heat and reflux for 4-9 hours, After cooling, add 20ml of nitric acid dropwise, stir at room temperature overnight after dropping, pour into crushed ice and stir to precipitate a solid, filter and wash with water to obtain an intermediate, which does not need to be dried for later use.

[0032] 2. Preparation of intermediate 2-methoxy-4-amino-5-nitrobenzoate sodium:

[0033] In the reaction bottle, add the intermediate obtained in the previous step, and then add aqueous sodium hydroxide solution to raise the temperature and reflux for 2-5 hours, then cool and filter to obtain the intermediate sodium 2-methoxy-4-amino-5-nitrobenzoate, which is directly used in the...

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Abstract

The present invention relates to alizapride hydrochloride preparing process, which includes the following steps: 1. preparing intermediate 2-methoxy-4-amino-5-nitrobenzoic acid; 2. preparing intermediate sodium 2-methoxy-4-acetamino-5-nitrobenzoate; 3. preparing intermediate 2-methoxy-4, 5-diaminobenzoic acid; 4. preparing intermediate 5-methoxy-6-carboxyl benzotriazole; 5. preparing intermediate 5-methoxy-6-methoxycarbonyl benzotriazole; and 6. preparing alizapride hydrochloride. The present invention has the advantages of high yield, simple operation and less pollution.

Description

technical field [0001] The invention belongs to the field of preparation of pharmaceutical raw materials, in particular to a preparation method of aripride hydrochloride. Background technique [0002] Alizapride hydrochloride (Alizapride hydrochloride) CAS: 59338-93-1, white powder, mp206~208℃. It is a powerful antiemetic drug, which can antagonize the emetic effect of apomorphine and dihydroergot alkaloids, etc., has a weak central nervous inhibitory effect without cholinergic effect, and is used to prevent and treat nausea and vomiting caused by tumor radiotherapy and chemotherapy . First listed in France in 1982, its chemical structure is as follows: [0003] [0004] At present, the preparation process of aripride hydrochloride at home and abroad mainly contains the following two kinds: [0005] 1. Using methyl p-aminosalicylate as the starting material to obtain the intermediate 5-methoxy-6-methoxycarbonylbenzotriazole through methyl etherification, protected nitr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12
Inventor 张广明孙乐大沈晓文
Owner 苏州摩尔医药有限公司
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