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Synthesis method of aniracetam

A synthetic method, the technology of aniracetam, which is applied in the field of drug synthesis, can solve the problems of using dangerous solvents and cumbersome operations, and achieve the effects of safe production, high yield, and maximized economic benefits

Inactive Publication Date: 2014-05-28
NORTHWEST UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The purpose of the present invention is to provide a new synthetic method of aniracetam with high product yield, safe production and comprehensive utilization of by-products to maximize economic benefits, so as to overcome the disadvantages of using dangerous solvents and complicated operations in the prior art

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  • Synthesis method of aniracetam
  • Synthesis method of aniracetam
  • Synthesis method of aniracetam

Examples

Experimental program
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Embodiment 1

[0014] Preparation of aniracetam: 17.0 g (0.2 mol) of α-pyrrolidone and 40.0 mL (0.28 mol) of triethylamine were dissolved in 100.0 mL of toluene. Control the temperature below 50°C and add dropwise 40 mL of toluene solution in which 34.2 g (0.2 mol) of p-methoxybenzoyl chloride is dissolved. After dripping, the water bath kept the temperature at 50°C for 2 hours. Pour the reaction solution into a 1000mL beaker, add 500mL of water, stir, filter with suction, and wash with water until the Cl ion of the washing solution is detected to be qualified, then dry the filter cake, and then recrystallize with ethanol to obtain white flaky crystals 37.2 g (84.7% yield). Melting point, 120.2-120.8°C.

[0015] Concentrate the above washing solution under reduced pressure (pressure less than -0.05MPa) to 1 / 4 of the volume of the original solution. The concentrated solution was lowered to room temperature, and 2 times the volume of ethanol was added for alcohol analysis to obtain 16.5 g o...

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Abstract

The invention discloses a synthesis method of aniracetam. The aniracetam is obtained by performing one-step reaction on alpha-pyrrolidone and methoxybenzoyl chloride in the existence of triethylamine serving as an acid-binding agent; after the reaction is completed, adding water into a product to remove triethylamine hydrochloride; concentrating water solution and performing alcohol extraction on the concentrated water solution to obtain the triethylamine hydrochloride. The synthesis method is safe in production and high in yield, and the economic benefit can be maximized by comprehensively utilizing byproducts.

Description

technical field [0001] The invention relates to a synthesis method of aniracetam, which belongs to the technical field of medicine synthesis. technical background [0002] Aniracetam, whose chemical name is 1-(4-methoxybenzoyl)-2-pyrrolidone, is a γ-lactam drug for improving brain function. It is mainly used clinically for the treatment of cerebrovascular sequelae, and can also be used for the elderly Dementia, enhance memory and protect the nervous system. Compared with other brain function improving drugs, it has the characteristics of strong effect, quick onset and low toxicity. [0003] Most of the synthesis methods of aniracetam at home and abroad use α-pyrrolidone and an electrophile to form an intermediate and then react with p-methoxybenzoyl chloride. In this way, not only the yield of aniracetam is low, but also sodium hydride is used. Such highly dangerous reagents, combined with cumbersome operation, are not suitable for industrialized large-scale production. ...

Claims

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Application Information

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IPC IPC(8): C07D207/263
CPCC07D207/263
Inventor 尹琰魏青
Owner NORTHWEST UNIV
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