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Process method for producing L-2-aminobutanamide hydrochloride serving as intermediate of levetiracetam

A technology of aminobutyramide and process method, which is applied in the direction of organic chemical method, carboxylic acid amide preparation, chemical instrument and method, etc. It can solve the problems of potential safety hazards, high temperature and pressure, high cost of desalination, etc., and achieve low raw material cost , short synthesis cycle, and the effect of controlling the production environment

Inactive Publication Date: 2010-12-29
HUANGGANG HUAYANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0022] When the hydantoin is hydrolyzed, the temperature and pressure are high, there are potential safety hazards, and a large amount of ammonia gas is released, and the cost of desalination is high

Method used

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  • Process method for producing L-2-aminobutanamide hydrochloride serving as intermediate of levetiracetam
  • Process method for producing L-2-aminobutanamide hydrochloride serving as intermediate of levetiracetam
  • Process method for producing L-2-aminobutanamide hydrochloride serving as intermediate of levetiracetam

Examples

Experimental program
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Embodiment Construction

[0034] Take L-2-aminobutyramide hydrochloride as an example:

[0035] The first step: use n-propionaldehyde as raw material to react with ammonia water, ammonium chloride and sodium cyanide to obtain 2-aminobutyronitrile.

[0036] 1. The ingredient ratio is:

[0037] Product name Dosage (g) Specification Remarks

[0038] Sodium cyanide 610 30%

[0039] Ammonia 530 25%

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Abstract

The invention discloses a process method for producing L-2-aminobutanamide hydrochloride serving as an intermediate of levetiracetam, which solves the problem that the conventional produced product has excessively high impurity content or production cost is too high for an enterprise to bear and the like. The method is characterized by comprising the following steps of: reacting propionaldehyde with ammonia water, ammonium chloride and sodium cyanide to obtain 2-amino butyronitrile; hydrolyzing the 2-amino butyronitrile under an alkali condition to obtain 2-aminobutanamide; and splitting the 2-aminobutanamide with L-tartaric acid to obtain the L-2-aminobutanamide hydrochloride. An L-2-amino amides product of which the content is over 99.5 percent is obtained by removing a byproduct, namely, sodium chloride by recrystallization so as to meet the use requirement of foreign customers. The process has the advantages of high yield, high safety and low cost and can be widely suitable for industrialized production of medium-sized and small enterprises.

Description

1. Technical field [0001] The invention belongs to the field of medicine and chemical industry, and relates to a preparation method of a drug intermediate, in particular to a process method of an intermediate L-2-aminobutyramide hydrochloride of a chemical antiepileptic drug levetiracetam . 2. Background technology [0002] L-2-aminobutanamide hydrochloride is an important intermediate of the antiepileptic drug levetiracetam (Levet iracetam is a pyrrolidone derivative). Approved by FDA, marketed in the United States. It is currently the only drug used to treat localized and secondary generalized epilepsy. The characteristics of this product are: 1. High therapeutic index; 2. It is a broad-spectrum therapeutic drug; 3. It is used in combination with other antiepileptic drugs without interaction; 4. It has two properties of antiepileptic and antiepileptic, which can prevent The occurrence of epilepsy (none of the currently available antiepileptic drugs on the market can pre...

Claims

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Application Information

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IPC IPC(8): C07C237/06C07C231/06C07B57/00
Inventor 姚文学刘志东
Owner HUANGGANG HUAYANG PHARMA
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