4-hydroxy-2-oxo-1-pyrrolidine acetamide racemate crystal I and preparation method thereof

A technology of pyrrolidine acetamide and racemate, which is applied in the field of 4-hydroxy-2-oxo-1-pyrrolidine acetamide medicine, and achieves the effects of being suitable for large-scale industrial production, high purity and remarkable curative effect

Active Publication Date: 2013-06-12
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But there is no relevant report on the racemate crystal form of 4-hydroxy-2-oxo-1-pyrrolidineacetamide

Method used

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  • 4-hydroxy-2-oxo-1-pyrrolidine acetamide racemate crystal I and preparation method thereof
  • 4-hydroxy-2-oxo-1-pyrrolidine acetamide racemate crystal I and preparation method thereof
  • 4-hydroxy-2-oxo-1-pyrrolidine acetamide racemate crystal I and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Dissolve 50mg of the crude racemate of 4-hydroxy-2-oxo-1-pyrrolidineacetamide in anhydrous methanol, stir overnight, filter, put the solution in a desiccator, and evaporate the solvent to obtain colorless transparent crystals , yield 82%, purity 99.4%.

[0047] The crude product of 4-hydroxyl-2-oxo-1-pyrrolidineacetamide racemate of the present invention is synthesized according to the following steps, and its purity is 98.5%:

[0048] (a) Add 139.6g of glycine ethyl ester hydrochloride into 1100ml of anhydrous ether, cool to -6°C and blow in 27.2g of ammonia gas to free glycine ethyl ester hydrochloride into glycine ethyl ester, wherein glycine ethyl ester hydrochloride Salt: anhydrous ether: 1mol of ammonia: 1100ml: 1.6mol;

[0049] (b) Add 336ml of absolute ethanol, 67.2g of sodium bicarbonate, and 166.6g of 4-chloro-3-hydroxy-butyric acid ethyl ester dropwise to the above product. The adding time is 1.8 hours. React at 72°C for 22 hours;

[0050] (c) Filtration, ...

Embodiment 2

[0054] Dissolve 100mg of the crude racemate of 4-hydroxy-2-oxo-1-pyrrolidineacetamide in 95% ethanol, stir overnight, filter, put the solution in a desiccator, and evaporate the solvent to obtain colorless transparent crystals , yield 85%, purity 99.2%.

Embodiment 3

[0056] Dissolve 50 mg of the crude racemate of 4-hydroxy-2-oxo-1-pyrrolidineacetamide in isopropanol, stir overnight, filter, and place the solution in a desiccator to evaporate the solvent to obtain colorless transparent crystals , yield 87%, purity 99.2%.

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Abstract

A crystal form I of the racemate of 4-hydroxy-2-oxo-1-pyrrolidine acetamide is prepared by the following steps: dissolving crude racemate of 4-hydroxy-2-oxo-1-pyrrolidine acetamide in a small molecular alcohol solvent to reach supersaturation; heating and stirring overnight at 38-42°C to obtain an suspended sediment; filtering and drying to obtain a crystal. The crystal form I of the racemate of 4-hydroxy-2-oxo-1-pyrrolidine acetamide in the present invention has a high purity which can reach 99.5%.

Description

technical field [0001] The invention relates to 4-hydroxy-2-oxo-1-pyrrolidineacetamide medicine, in particular to 4-hydroxy-2-oxo-1-pyrrolidineacetamide racemate crystal form I and a preparation method thereof. Background technique [0002] 4-Hydroxy-2-oxo-1-pyrrolidineacetamide is a new generation of brain metabolism improving drugs, pyrrolidone (cyclic GABOB) derivatives, piracetam analogs, can promote the synthesis of phosphorylcholine and o-acethanolamine , promote brain metabolism, stimulate specific central nervous pathways through the blood-brain barrier, and improve intelligence and memory. It has a good curative effect on cerebrovascular disease, brain injury, brain tumor (postoperative), intracranial infection, dementia, and brain degenerative diseases. It is suitable for memory and intellectual impairment caused by mild to moderate vascular dementia, senile dementia and traumatic brain injury. 4-Hydroxy-2-oxo-1-pyrrolidineacetamide was first synthesized in 1974 ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/273
CPCC07D207/273
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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