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Method suitable for industrial production of memantine hydrochloride

A technology for memantine hydrochloride and dimethyladamantane, which is applied in the field of medicine, can solve the problems of difficult handling of aluminum reagents, unfavorable industrialization and the like, and achieves the effects of simplified post-processing process, easy post-processing and high yield

Inactive Publication Date: 2017-11-21
CHANGZHOU PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0027] This route has a high yield, but it is difficult to handle the aluminum reagent used, which is not conducive to industrialization

Method used

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  • Method suitable for industrial production of memantine hydrochloride
  • Method suitable for industrial production of memantine hydrochloride
  • Method suitable for industrial production of memantine hydrochloride

Examples

Experimental program
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Effect test

Embodiment

[0043] (1) Preparation of 1-acetylamino-3,5-dimethyladamantane

[0044] Add 1,3-dimethyladamantane (300kg) and acetonitrile (1.18kg) into the reaction flask, start stirring, heat in a water bath to 60°C-65°C, pump concentrated sulfuric acid (5.37kg) into the high level tank, add dropwise Concentrated sulfuric acid, the temperature will rise, control the rate of addition, and keep the temperature in the bottle not higher than 75°C. After the dropwise addition, keep the temperature of the reaction bottle at 70°C to 80°C, stir and react for 18 hours, then cool to 20°C to 30°C, slowly pump the reaction solution into a 50L reaction kettle with 20kg of ice water (inner Temperature control 0°C~10°C), after the addition, add dichloromethane (10kg) for extraction, separate the liquid, wash the organic phase (lower layer) with purified water twice, 4kg each time, transfer the dichloromethane to In a distillation flask, concentrate under reduced pressure (the vacuum degree of the water ...

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PUM

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Abstract

The invention relates to a method suitable for industrial production of memantine hydrochloride. 1,3-dimethyl adamantane is used as a starting material, and a Ritter reaction, hydrolysis, salt forming and refining are used for preparing; during the Ritter reaction, acetonitrile is directly used as an acetylation reagent, concentrated sulfuric acid is used as a catalyst and a solvent, and the reaction is carried out at 70-80 DEG C; after the reaction ends, water is directly added into ice water, dichloromethane is used for extraction and drying by distillation, n-hexane is used for recrystallization, and 1-acetamido-3, 5-dimethyladamantane is directly obtained by one step; 1-acetamido-3, 5-dimethyladamantane is hydrolyzed under an alkaline condition in order to obtain 1-amino-3, 5-dimethyladamantane, a memantine crude product is obtained by salt forming of 1-amino-3, 5-dimethyladamantane under the condition of dichloromethane solvent acidifying, water is used as a solvent in order to carry out recrystallization of the crude product, and a refined product is obtained. In the first acetyl amination process, concentrated sulfuric acid is used as a catalyst and a solvent, tedious industrial post-treatment due to usage of anhydrous aluminium chloride as a catalyst is avoided, an extractant employs dichloromethane, in order to avoid usage of chloroform of high toxicity, and recrystallization employs water as a solvent with environmental protection and cost saving.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a method for industrialized production of raw material memantine hydrochloride. Background technique [0002] As early as 1982, memantine was listed in Germany under the trade name Akatinol by Merz Company as a drug for the treatment of dementia, and it has been listed in other countries successively. Companies such as Merz, Lundbeck, and NTI have also used the drug in research on the treatment of Alzheimer's disease (AD) and AIDS-related dementia. On February 20, 2002, the European Patent Medicines Committee (CPMP) approved the memantine hydrochloride of Lundbeck Company (transferred from Merz Pharma Company) for the treatment of moderate and severe senile dementia patients. In 2010, the memantine sustained-release preparation developed by Forest Labs was approved by the US FDA. my country approved the import of memantine hydrochloride tablets from foreign pharmaceutical companies in S...

Claims

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Application Information

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IPC IPC(8): C07C209/00C07C211/38C07C209/84C07C231/06C07C233/06
CPCC07C209/00C07C209/62C07C209/84C07C231/06C07C233/06C07C211/38
Inventor 王仁冬金晓峰巫美金
Owner CHANGZHOU PHARMA FACTORY
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