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Oxiracetam medicinal composition, and preparation method and application thereof

A technology of oxiracetam and its composition, which is applied in the field of oxiracetam pharmaceutical composition and its preparation, and can solve the problems of harming the health of the drug, invalid active ingredients of the drug, toxic and side effects, etc.

Inactive Publication Date: 2013-09-18
LIAONING YILING KECHUANG BIOLOGICAL MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Because oxiracetam is easy to produce some by-products and impurities during the synthesis process, the obtained compound drug is not a pure substance, so that the active ingredient of the drug has invalid, antagonistic or even toxic and side effects substances, which affects the therapeutic effect and endangers the health of the drug.

Method used

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  • Oxiracetam medicinal composition, and preparation method and application thereof
  • Oxiracetam medicinal composition, and preparation method and application thereof
  • Oxiracetam medicinal composition, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Preparation of ethyl 2-(2-pyrrolidin-2,4-dione-1-yl)acetate

[0045] Add 80.0kg (308.6mol) of ethyl 2(3-ethoxyformyl-4-hydroxypyrrolidin-2-one-1-yl)acetate, 800L of acetonitrile, and 7.2L of water into the reaction tank, stir and dissolve, then heat Reflux for 20min. The solution was distilled to dryness under reduced pressure. The residue was dissolved in 300L of hot isopropanol, added with 3.0kg of activated carbon for decolorization for 30min, filtered, the filtrate was cooled to room temperature, centrifuged, and dried.

[0046] 50.2 kg of ethyl 2-(2-pyrrolidin-2,4-dione-1-yl)acetate was obtained.

[0047] Yield 87.8% mp87-91℃

Embodiment 2

[0049] Preparation of ethyl 2-(4-hydroxypyrrolidin-2-one-1-yl)acetate

[0050] Add 50.2kg (271.0mol) of ethyl 2-(2-pyrrolidin-2,4-dione-1-yl)acetate and 600L tetrahydrofuran into the reaction tank, stir and dissolve, cool to 0°C, add sodium borohydride 3.42kg (90.4mol). Stir at 0-5°C for 10 minutes, then at room temperature for 30 minutes. Adjust the pH value to 2.5-3.0 with concentrated hydrochloric acid, drop it in about 1 hour, filter, and distill the filtrate to dryness under reduced pressure. Dissolve the residue in 260L of hot isopropanol, add 3.0kg of activated carbon to decolorize for 30min, filter, cool the filtrate to room temperature, centrifuge, and shake dry.

[0051] 42.8kg of ethyl 2-(4-hydroxypyrrolidin-2-on-1-yl)acetate was obtained.

[0052] Yield 84.8% mp 180°C (dec).

Embodiment 3

[0054] Preparation of Oxiracetam

[0055] Add 42.8kg (228.8mol) of ethyl 2-(4-hydroxypyrrolidin-2-one-1-yl)acetate and 860L of methanol into the reaction kettle, stir and dissolve, cool down to 0°C, and feed ammonia gas until Saturated, left overnight (> 20 hours), under reduced pressure distillation to recover ammonia and solvent, the resulting viscous.

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Abstract

The invention discloses an oxiracetam medicinal composition having a high safety, and a preparation method and an application thereof. The medicinal composition contains oxiracetam and below 0.5% of a compound having a structure represented by formula II. A case that 4-hydroxy-2-oxo-1-pyrrolidineaceticacid is the largest-content impurity in the oxiracetam compound is proved for the first time, purifying characterization and relevant researches on 4-hydroxy-2-oxo-1-pyrrolidineaceticacid are carried out, and the researches find that 4-hydroxy-2-oxo-1-pyrrolidineaceticacid is related with the side effects of the oxiracetam medicine and can cause a series of untoward effects. The oxiracetam medicinal composition has a high safety. The invention further provides the preparation method of the oxiracetam medicinal composition.

Description

technical field [0001] The invention belongs to nootropic drugs, in particular to an oxiracetam pharmaceutical composition and its preparation method and application. Background technique [0002] Oxiracetam (shown in formula I), is the analog of piracetam, is a kind of synthetic hydroxyaminobutyric acid (GABOB) cyclic derivative, can promote the synthesis of phosphorylcholine and phosphorylethanolamine, improve The ratio of ATP / ADP in the brain can enhance the conduction of nerve excitation, improve the retrograde amnesia caused by hypoxia, and can enhance memory. It can improve the memory and learning function of patients with senile dementia and memory impairment. [0003] Nootropic drugs selectively act on the cerebral cortex, and have the characteristics of selectively activating, protecting and promoting the recovery of damaged nerve cell functions, and have no calming and exciting effects. At present, the clinical drugs for the treatment of cognitive dysfunction inc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4015A61P25/28G01N33/15
Inventor 关屹闫冬
Owner LIAONING YILING KECHUANG BIOLOGICAL MEDICAL TECH
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