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Preparation method of drug nefiracetam for treating Alzheimer's disease

A technology of nefiracetam and a synthesis method, which is applied in the field of western medicine synthesis, can solve the problems of long reaction route of nefiracetam, expensive raw materials, low product purity, etc., and achieves high yield, easy reaction process, and reaction selectivity. strong effect

Active Publication Date: 2021-11-16
THE SECOND PEOPLES HOSPITAL OF SHENZHEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] The technical problem to be solved in the present invention is aimed at the problems in the prior art that the reaction route of nefiracetam is relatively long, some reaction conditions are relatively harsh, the price of raw materials is relatively expensive, the yield is low, and the purity of the product is not high.

Method used

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  • Preparation method of drug nefiracetam for treating Alzheimer's disease
  • Preparation method of drug nefiracetam for treating Alzheimer's disease
  • Preparation method of drug nefiracetam for treating Alzheimer's disease

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[0023] The invention discloses a preparation method of nefiracetam, and those skilled in the art can learn from the content of this article and appropriately improve the process parameters to realize it. It needs to be pointed out that all similar replacements and modifications are obvious to those skilled in the art, and they are all considered to be included in the present invention, and relevant personnel can obviously make changes without departing from the content, spirit and scope of the present invention. Changes or appropriate changes and combinations are made to the content described herein to realize and apply the technology of the present invention.

[0024] In the present invention, unless otherwise specified, the scientific and technical terms used herein have the meanings commonly understood by those skilled in the art.

Embodiment 1

[0027] In 250 mL of tetrahydrofuran, add 14.3 g (about 0.1 mol) of 2-oxopyrrolidine acetic acid, 17.7 g (about 0.11 mol) of CDI and 20.2 g (about 0.2 mol) of triethylamine, heat to 40 ° C, and react for 1.5 hours. obtaining a solution containing the intermediate compound;

[0028] Add 13.3 grams (about 0.11mol) of 2,6-dimethylaniline directly into the above solution, keep it warm for half an hour, monitor the reaction progress by TLC, add 150mL water for extraction after the reaction is completed, and wash the organic phase twice with saturated sodium chloride water , dried over anhydrous magnesium sulfate, concentrated under reduced pressure, and subjected to column chromatography, the eluate was concentrated to remove the solvent, and dried in vacuo to obtain 24.0 g (about 0.0974 mol) of nefiracetam product with an HPLC purity of 99.81%.

Embodiment 2

[0030] In 250 mL of dichloromethane, add 14.3 g (about 0.1 mol) of 2-oxopyrrolidine acetic acid, 17.7 g (about 0.11 mol) of CDI and 23.7 g (about 0.3 mol) of pyridine, heat to 35 ° C, and react for 1.5 hours. obtaining a solution containing the intermediate compound;

[0031] Add 14.5 g (about 0.12 mol) of 2,6-dimethylaniline directly into the above solution, keep it warm for half an hour, monitor the reaction progress by TLC, add 150 mL of water for extraction after the reaction is completed, and wash the organic phase twice with saturated sodium chloride water , dried over anhydrous magnesium sulfate, concentrated under reduced pressure, dissolved in ethanol, cooled and crystallized at 0°C, filtered, and vacuum-dried to obtain 23.9 g (about 0.097 mol) of nefiracetam product with an HPLC purity of 99.88%.

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Abstract

The invention belongs to the field of western medicine synthesis, and specifically discloses a preparation method of nefiracetam, a medicine for treating Alzheimer's disease. The preparation method activates the carboxyl group in 2-oxopyrrolidine acetic acid by N'N-dicarbonylimidazole (CDI), increases the reactivity, improves the reaction rate, reduces the occurrence of side reactions, and obtains a high product yield. The purity is high, the production cost is reduced, and it is beneficial to industrialized production.

Description

technical field [0001] The application relates to a preparation method of nefiracetam, a medicine for treating Alzheimer's disease, and belongs to the field of western medicine synthesis. Background technique [0002] As the world's population ages, the quality of life of the elderly has become a growing concern. Dementia is a major contributor to the decline in the quality of life of the elderly. It is a progressive neurodegenerative disease with insidious onset. Clinically, it is characterized by comprehensive dementia such as memory impairment, aphasia, apraxia, agnosia, impairment of visuospatial skills, executive dysfunction, and personality and behavior changes. The etiology is still unknown. It can be divided into Alzheimer's disease (AD), vascular dementia (VD), Lewy body dementia, Parkinson's disease dementia, Pick's disease, motor neuron disease, etc., among which AD is the most common. Medical research has found that the pathology of AD is mainly manifested as:...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D207/27
CPCC07D207/27
Inventor 谭回李维平黄国栋
Owner THE SECOND PEOPLES HOSPITAL OF SHENZHEN
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