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Preparation method of acipimox

A technology of carboxylic acid and methylpyrazine, which is applied in the field of medicine and chemical industry, can solve the problems of high technical requirements, high production cost, and low yield, and achieve the effects of economical and environmentally friendly yield, improved efficiency, and low reaction temperature

Pending Publication Date: 2020-12-25
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] In order to solve the problems of low yield and low purity in the preparation process of acipimox in the prior art; high technical requirements, serious environmental pollution and high production cost, the invention provides a new method for preparing acipimox. The method is novel, the raw materials are readily available, the operation is simple, the reaction is milder, the economy is environmentally friendly and the yield is high, and it is suitable for industrial production

Method used

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  • Preparation method of acipimox

Examples

Experimental program
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Effect test

Embodiment 1

[0034]Weigh 50.0g of 5-methylpyrazine-2-carboxylic acid, add it to 100.0ml purified water, add 40.0g of concentrated hydrochloric acid, stir for 30min, add 38.5g peroxyacetic acid, stir at room temperature for 3h, use 50% after the reaction is over The pH value of the sodium hydroxide solution was adjusted to 4.0, the temperature of the reaction solution was cooled to 5°C to precipitate crystals of asimimus, which were filtered off with suction and washed with water (20ml), and dried under vacuum at 50°C to obtain asimimus with a yield of 98.5% and a purity of 99.98%.

Embodiment 2

[0036]Weigh 50.0g of 5-methylpyrazine-2-carboxylic acid, add it to 100.0ml purified water, add 30.0g of concentrated hydrochloric acid, stir for 30min, add 38.5g of peracetic acid, stir at room temperature for 2h, and use 50% hydrogen for the end of the reaction The potassium oxide solution was adjusted to pH 4.0, the temperature was lowered to 5°C to precipitate crystals of asimimus, which was filtered with suction, washed with water (20ml), and dried under vacuum at 40°C to obtain asimimus with a yield of 94.5% and a purity of 99.94%.

Embodiment 3

[0038]Weigh 50.0g of 5-methylpyrazine-2-carboxylic acid, add it to 100.0ml purified water, add 25.0g of concentrated hydrochloric acid, stir for 30min, add 31.4g of peroxyformic acid, stir and react at room temperature for 2h, use 50% sodium hydroxide The pH value of the solution was adjusted to 4.0, and the temperature was lowered to 5°C to precipitate crystals of asimimus. After suction filtration, the crystals were washed with water (20ml), and dried under vacuum at 50°C to obtain asimimus with a yield of 92.3% and a purity of 99.89%.

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Abstract

The invention belongs to the field of pharmaceutical chemicals, and particularly relates to a preparation method of acipimox. The method for preparing acipimox comprises the following steps of adding5-methylpyrazine-2-carboxylic acid into purified water, adding concentrated hydrochloric acid for salifying, adding an oxidant, cooling and crystallizing to obtain the acipimox. The method has the advantages of simple reaction conditions, high selectivity in the nitrogen oxide formation process, avoiding of the use of a metal catalyst, simplification of the preparation process, effective improvement of the yield and the purity of the acipimox, and suitableness for industrial production.

Description

Technical field[0001]The invention belongs to the field of medicine and chemical industry, and specifically relates to a preparation method of asimimus.Background technique[0002]The chemical name of Acipimox (Acipimox) is 5-methylpyrazine-2-carboxylic acid-4-oxide. It is a niacin derivative developed by Pfizer Pharmaceuticals. It can inhibit the decomposition of adipose tissue and reduce The release of free fatty acids reduces the synthesis of triacylglycerols, and reduces the content of plasma total cholesterol, triglycerides, low-density lipoprotein and very low-density lipoprotein, and increases the content of high-density lipoprotein, which has a lasting and stable effect. Mainly used for the treatment of hypertriglyceridemia (type IV), hypercholesterolemia type IIa and IIb, type III and type V hyperlipoproteinemia. It is particularly effective for hyperlipidemia patients with gout and diabetes. The structure is as follows:[0003][0004]At present, the synthesis of asimimus is mai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D241/24
CPCC07D241/24
Inventor 许建国臧超
Owner LUNAN PHARMA GROUP CORPORATION
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