Improved process for the manufacture of moxonidine

A mixture and technology within minutes, applied in the direction of organic chemistry, etc., can solve the problems of no public synthesis method of moxonidine

Inactive Publication Date: 2015-12-02
FARMAK
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0029] Furthermore, the prior art literature does not disclose a method for the synthesis o

Method used

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  • Improved process for the manufacture of moxonidine
  • Improved process for the manufacture of moxonidine
  • Improved process for the manufacture of moxonidine

Examples

Experimental program
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Example

[0053] Preparation Examples 1 to 3 Preparation of Moxonidine

[0054] 102 kg (128 L, 3014.4 mol) of methanol and 7.7 kg (55.6 mol) of potassium carbonate were injected into the reactor, and the mixture was vigorously stirred and heated to 65°C. 8kg DMAIA (27.8mol) was divided into 8 portions and added within 20 minutes. The contents of the reactor were kept at 65°C with stirring for an additional 7 to 12 minutes. The reaction was stopped by transferring the entire reaction mixture to a separate pre-cooled reactor in less than 1 minute and further cooling the reaction mixture to below 25°C in 20 minutes.

[0055] work process:

[0056] The pH value is adjusted to pH≤7 with acetic acid. The reaction mixture is optionally filtered through activated carbon. Then the pH of the filtrate was adjusted to pH ≥ 8 with aqueous ammonia solution, and moxonidine was separated, washed with water and methanol, and dried.

[0057] Yield: Theoretically 92.0%

[0058] Table 1: Moxonidine impuritie...

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Abstract

The present invention describes a novel process for the preparation of Moxonidine (Formula (I)).

Description

technical field [0001] The present invention relates to a new process for the preparation of Moxonidine. Background technique [0002] 4-Chloro-N-(imidazolidine-2-ylidene)-6-methoxy-2-methylpyrimidin-5-amine has the International Nonproprietary Name (INN) Moxonidine and is used as an antihypertensive agent. It has the structural formula (I): [0003] [0004] Moxonidine can be obtained by key intermediate, 4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazoline-2-yl) aminopyrimidine (hereinafter referred to as DMAIA) of structural formula (II) )preparation: [0005] [0006] US Patent No. 4,323,570 discloses a process for preparing moxonidine (I) by reacting a compound of formula (II) with sodium methoxide. [0007] In CZ294649, the preparation of moxonidine from DMAIA by a reaction using an alkali metal carbonate in methanol is disclosed. [0008] EP1873151 proposes the use of bases such as sodium hydroxide and potassium hydroxide for the reaction with DMAIA. [0009] A ...

Claims

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Application Information

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IPC IPC(8): C07D403/12
CPCC07D403/12
Inventor 扬·诺沃提尼帕维尔·赫拉迪尔卢博米尔·克瓦皮尔马丁·格雷普尔彼得·什莱扎尔扎德克·梅尔尼茨基
Owner FARMAK
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