Method for large-scale preparation of pramiracetam

A technology of pramiracetam hydrate and tetrahydrofuran, which is applied in the field of fine chemical product production to achieve the effects of low environmental pollution, low cost and high purity

Inactive Publication Date: 2013-04-03
KAMP PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The present invention aims to overcome the deficiencies of the existing pramiracetam synthesis process, to provide a high yield, safe, pollution-free, low cost, ...

Method used

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  • Method for large-scale preparation of pramiracetam
  • Method for large-scale preparation of pramiracetam
  • Method for large-scale preparation of pramiracetam

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Experimental program
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Embodiment Construction

[0027] The following implementation is only to illustrate the present invention in more detail, but does not limit the present invention in any form.

[0028] The preparation method of pramiracetam:

[0029] (1) Synthesis of N-(2-(diisopropyl)ethyl)-2-chloroacetamide hydrochloride (Intermediate A):

[0030] Take a dry 1000ml three-neck bottle, install mechanical stirring, dropping funnel, and thermometer. Add 72g (0.5mol) of diisopropylethylenediamine and 500ml of dry tetrahydrofuran, and stir the reaction at about 315 rpm. Ice bath, starting at 2°C. Slowly add 45ml (0.56mol) of chloroacetyl chloride dropwise. When the dropwise addition was carried out for about one hour, a yellow sticky substance formed on the wall. Speed ​​up the rotating speed to about 350 rpm, and continue the dropwise addition reaction. The temperature of the whole reaction process was controlled within 15°C. After about one hour and forty minutes, the dropwise addition was completed, and th...

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Abstract

The invention relates to a method for large-scale preparation of pramiracetam. The method comprises the following steps of: carrying out a condensation reaction, dissolving and filtering, re-dissolving and extracting, refluxing, freezing and suction-filtering. The method provided by the invention has simple process operation, is safe and pollution-free. Moreover, the prepared pramiracetam has high yield, high purity, easily obtained materials, and low production cost, and is suitable for large-scale production of the enterprises.

Description

technical field [0001] The invention belongs to the production field of fine chemical products, and in particular relates to a preparation process of pramiracetam, which is used for producing medicines for improving brain function. Background technique [0002] Pramiracetam was first listed in Italy in 1993. Its chemical name is N-(2-(diisopropylamino)ethyl)-2-oxo-1-pyrrolidineacetamide. Tan analogues, new pyrrolidone-like brain function improvers, suitable for memory and recognition impairment, language disorders and Alzheimer's syndrome (Alzheimer's disease), its chemical structure is shown in Figure I . [0003] In the literature [Peng Zhenyun, Sun Yongju, Qi Chao, Synthesis of Pramiracetam, China Pharmaceutical Industry, 1998, 29 (8): 344] obtained by reacting ethyl pyrrolidone acetate and N,N-diisopropylethylenediamine . Pyrrolidone ethyl acetate is obtained from the sodium salt of pyrrolidone according to the Gabriel synthesis. In the ammonolysis reaction, an exces...

Claims

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Application Information

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IPC IPC(8): C07D207/27
Inventor 曾培安张浩吴锋刘娟张静吴健民贺莲
Owner KAMP PHARMA
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