Production method of acipimox

A production method and the technology of maleic anhydride are applied in the production field of acyclolimus, can solve problems such as high manufacturing cost and complicated production, and achieve the effects of low manufacturing cost and convenient production

Inactive Publication Date: 2015-07-01
储海燕
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  • Abstract
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  • Claims
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Problems solved by technology

As currently in the production of acipimox, the manufa

Method used

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Embodiment Construction

[0006] Now in conjunction with the present invention for further detailed description.

[0007] A kind of production method of acipimox of the present invention, concrete steps are as follows: under cooling and stirring, in the solution that 78g maleic anhydride is dissolved in 60ml chloroform, add the hydrogen peroxide of 40ml30%, add 4.8g again after 2h 5-Methylpyrazine-2-carboxylic acid, kept at 0-5°C for 2 days, filtered off the maleic acid, concentrated to a small volume, added ethyl acetate, filtered to obtain 1.1g of acipimox, melting point 178~180℃.

[0008] Acilimus can inhibit the release of free fatty acids from adipose tissue, reduce blood very low-density lipoprotein and low-density lipoprotein, thereby reducing the concentration of triglyceride and cholesterol in blood, and can also promote the increase of high-density lipoprotein. For ⅡA, Ⅱ R, Ⅲ, Ⅳ and V hyperlipoproteinemia; blood lipid-lowering drugs.

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Abstract

The invention relates to a production method of acipimox, wherein the production method comprises the following specific steps: under cooling and stirring, dissolving 78 g of maleic anhydride in 60 ml of a chloroform solution, adding 40 ml of a 30% hydrogen peroxide, 2 h later, adding 4.8 g of 5-methylpyrazine-2-carboxylic acid, keeping for 2 d at the temperature of 0-5 DEG C, filtering to remove maleic acid, concentrating to leave small volume, adding ethyl acetate, and filtering to obtain 1.1 g of acipimox with the melting point of 178-180 DEG C. According to the production method of acipimox, the manufacturing cost is low, and the production is convenient.

Description

technical field [0001] The invention relates to the field of medicine manufacture, in particular to a production method of acipimox. Background technique [0002] Acilimus is used for various primary and secondary hyperlipidemia, can reduce plasma total cholesterol, triglyceride, low-density lipoprotein and very low-density lipoprotein content, and increase high-density lipoprotein content. Long-lasting and stable. This product can be used not only as the preferred lipid-lowering drug to treat mild hyperlipidemia, but also as a basic lipid-lowering drug, which can be used in combination with other lipid-lowering drugs to improve the curative effect. This product can still be used as a hypoglycemic drug and play an auxiliary role in the treatment of diabetes. In addition, this product can also be used as an antioxidant drug. Since it is currently in the production of acipimox, the manufacturing cost is high and the production is complicated. Contents of the invention ...

Claims

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Application Information

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IPC IPC(8): C07D241/24
CPCC07D241/24
Inventor 储海燕
Owner 储海燕
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