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A kind of preparation method of milbe oxime

A technology of mirbeoxime and mirbeone, applied in the field of medicine, can solve the problems of low production efficiency, adverse health effects of process executors, etc.

Active Publication Date: 2021-05-07
LIVZON GROUP FUZHOU FUXING PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since both dioxane and methanol are highly toxic solvents, it is easy to cause adverse effects on the health of process executors, and because the reaction time takes 12 hours, the production efficiency is extremely low

Method used

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Experimental program
Comparison scheme
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Embodiment Construction

[0007] In order to describe the technical content, achieved objectives and effects of the present invention in detail, the following descriptions will be made in conjunction with the embodiments.

[0008] The most critical idea of ​​the present invention is: replacing highly toxic dissolved coal with a low-toxic solvent, which greatly reduces the occupational health hazards of this step to employees; the reaction time is greatly shortened, and production efficiency is improved.

[0009] A preparation method of milbexime comprises the following steps: dissolving milbetone with ethyl acetate-ethanol solution as a reaction solvent, adding hydroxylamine hydrochloride aqueous solution and reacting for 4-6 hours to prepare milbexime.

[0010] As can be seen from the above description, the beneficial effect of the present invention is: adopting the method of the present invention to prepare milbexime can completely convert milbetone into milbexime, and the yield can reach more than 99...

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PUM

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Abstract

The invention discloses a preparation method of milbexime, which comprises the following steps: dissolving milbetone with ethyl acetate-ethanol solution as a reaction solvent, adding hydroxylamine hydrochloride aqueous solution and reacting for 4-6 hours to prepare milbexime. The preparation method also includes the step of purifying the prepared milbexime, and the purification step is specifically: washing the prepared milbexime with water, dissolving it in ethanol, adding it dropwise to water for crystallization under stirring, Filter and dry to obtain pure milbexime. Compared with the prior art, the preparation method uses a low-toxic solvent to replace high-toxic dissolved coal, which greatly reduces the occupational health hazards of this step to employees; the reaction time is greatly shortened, and the production efficiency is improved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of milbexime. Background technique [0002] Milbemycin is an oxime derivative of milbemycin A3 and A4, a macrolide anti-endoparasite drug. Milbexime has a broad-spectrum anti-parasitic effect, and has a good killing effect on internal and external parasites, especially nematodes and arthropods. It is usually used to prevent dirofilariasis and control dogs and cats caused by nematodes and hookworms. Diseases and canine whipworm disease, etc. [0003] In the prior art, dioxane and methanol are usually used as solvents to dissolve milbetone, and then react with hydroxylamine hydrochloride to obtain milbexime. However, since both dioxane and methanol are highly toxic solvents, they are likely to cause adverse effects on the health of process executors, and because the reaction time needs to be 12 hours, the production efficiency is extremely low. Contents of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/22
CPCC07D493/22
Inventor 刘小刚刘文锋梁倍陈明渝
Owner LIVZON GROUP FUZHOU FUXING PHARMACEUTICAL CO LTD