Method of preparing 4-hydroxy pyrrolidone-2-acetylamine

A technology of hydroxypyrrolidone and hydroxybutanone aminoacetamide, which is applied in the field of preparing 4-hydroxypyrrolidone-2-acetamide, can solve the problems that the purity cannot be fully used in medicine, cannot meet industrial scale production, and the product components are complex, etc. The effect of cheap raw materials, low cost, and easy availability of raw materials

Inactive Publication Date: 2007-04-18
SUZHOU HOPE TECH
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  • Abstract
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  • Application Information

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Problems solved by technology

However, in this method, there are many side reactions, and the composition of the final product is very complicated. After refining, its purity cannot fully meet the requirements for medical use.
In addition, the reaction time is very long, needing more than 20 hours, and its final yield is very low, which cannot meet the needs of industrial scale production

Method used

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  • Method of preparing 4-hydroxy pyrrolidone-2-acetylamine
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  • Method of preparing 4-hydroxy pyrrolidone-2-acetylamine

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Embodiment Construction

[0018] The present invention will be described in more detail with examples below, but it cannot be considered that the present invention is limited to this example.

[0019] 1. Preparation of chloroacetoacetyl chloride

[0020] 500 ml of dichloromethane and 86 g of diketene (1.0 mol, purity 98%) were added to the reactor. The mixture was cooled to -10~-20°C while stirring, and 71 g (1.0 mol) of chlorine gas was introduced to react for 2 hours. Chloroacetoacetyl chloride was obtained by gas chromatography analysis.

[0021] 2. Preparation of chloroacetoacetamidoacetamide

[0022] Naturally warm up the chloroacetoacetyl chloride solution synthesized above to -10~0°C, add glycinamide hydrochloride 112g (1.0mol, purity 98.5%) in batches to this mixed solution while stirring, and keep warm for 2 Hour. Dichloromethane was recovered by distillation under reduced pressure, and the distillation residue was washed with ethanol to obtain 177.6 g (yield 90.8%) of the target product, ...

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Abstract

The present invention discloses a preparation method of oxiracetam (4-hydroxypyrrolidone-2-acetylamine) which can be used as cerebral function improving agent. Said method uses diketene as initial raw material, and includes the following steps: firstly, making the diketene be reacted with chlorine gas to obtain chloroacetoacetyl chloride, then making the chloroacetoacetyl chloride undergo the processes of substitution, hydrogenation and cyclopolymerization, etc. so as to obtain the invented product.

Description

technical field [0001] The invention relates to a method for preparing 4-hydroxypyrrolidone-2-acetamide. Background technique [0002] 4-Hydroxypyrrolidone-2-acetamide, commonly known as oxiracetam, is used in medicine as a brain function improver. [0003] In Japanese Patent JP62026267, it is proposed to directly react 3-hydroxy-4-halogenated butyric acid derivatives with glycinamide to prepare the target product oxiracetam. However, in this method, there are many side reactions, and the composition of the final product is very complicated. After refining, its purity cannot fully meet the requirements for medical use. In addition, the reaction time is very long, more than 20 hours, and its final yield is very low, which cannot meet the needs of industrial scale production. Contents of the invention [0004] The technical problem to be solved by the present invention is to provide a method for preparing oxiracetam with lower cost, higher yield and simple operation. [0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/273
Inventor 陈小萍黄卫一夏秋霞刘纪才
Owner SUZHOU HOPE TECH
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