Purification method for moxidectin

A purification method and crude product technology, applied in the field of medicinal chemistry, can solve problems such as low yield, high cost, and long production cycle, and achieve the effects of high yield, low cost, and short crystallization time

Inactive Publication Date: 2015-10-28
XINYU PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method takes a long time, the yield is low, and the product purity is not significantly improved; ②The column chromatography purification method mentioned in the Chinese patent CN101372492A, this method can obtain moxidectin with a purity of more than 90%, but consumes a large amount of organic Solvent, the production cycle is long, resulting in high cost and low production capacity; ③ the methods disclosed in US Pat

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Put crude moxidectin (10g, purity 92%), methanol 10mL, 2,6-

[0028] 0.1g of di-tert-butyl-4-methylphenol, heated up to 60°C, stirred until dissolved; then added 30g of n-heptane,

[0029] Then lower the temperature by 6-8°C per hour, drop the temperature to 10°C, filter, and rinse the filter cake with 10°C n-heptane. The filter cake was vacuum-dried at 80°C for 20 hours to obtain high-purity moxidectin with a yield of 81.0% and a purity of 97.5%.

Embodiment 2-4

[0030] Embodiment 2-4: Other process conditions and experimental steps are the same as in Embodiment 1, but use different weights of dissolving agent n-heptane, and the experimental results are shown in Table 1. It is proved that n-heptane is 3 times the weight of the crude product of moxidectin and has the highest purity. The eluent can also be selected from n-hexane, and the effect and result are similar, so no more examples are given here.

[0031] Table 1 Crystallization results using different weights of n-heptane

[0032] project n-heptane weight / g Moxidectin yield / % purity / % Example 2 30 81.0 97.5 Example 3 45 87.2 97.0 Example 4 60 90.3 95.2

Embodiment 5-7

[0033] Examples 5-7: Other process conditions and experimental steps are the same as in Example 1, but different solvents are used, and the experimental results are shown in Table 2. Prove that ethanol is used as a solvent, and the product has the highest purity.

[0034] Table 2 Crystallization results using different solvents

[0035] project solvent Moxidectin yield / % purity / % Example 5 ethanol 76.2 98.4 Example 6 n-propanol 72.4 97.3 Example 7 Isopropanol 70.5 96.2

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PUM

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Abstract

The invention provides a purification method for moxidectin. The purification method comprises the steps: mixing a moxidectin crude product with a solvent and adding an antioxidant; stirring the mixture at 60-80 DEG C to prepare a solution; and then adding a solventing-out reagent and finally drying mixture under the vacuum condition through cooling crystallization to obtain high purity moxidectin with the purity being over 96%. The purification method for moxidectin provided by the invention has the advantages of short crystallization time, low cost and high yield and provides a novel method for improving the purity of moxidectin.

Description

technical field [0001] The invention provides a method for purifying moxidectin, which belongs to the field of medicinal chemistry. Background technique [0002] Moxidectin is a semi-synthetic single-component macrolide antibiotic produced by the fermentation of Streptomyces, and it is a derivative of nimoxectin. Macrolide antiparasitic drugs consist of two major classes, abamectins and milbemycins. Compared with ivermectin and avermectin, moxidectin has wider anthelmintic activity, long-term effect and safety characteristics. In the mid-1980s, moxidectin began to be used as an anthelmintic for animals. As a new generation of anthelmintic drug, moxidectin can effectively kill nematodes and ectoparasites, and has good safety to animals. It is superior to ivermectin in terms of dosage, dosage form development, drug resistance and drug distribution in vivo. At present, moxidectin is a broad-spectrum, high-efficiency, new macrolide anthelmintic antibiotic widely used in vete...

Claims

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Application Information

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IPC IPC(8): C07D493/22
CPCC07D493/22
Inventor 丁振东王珍肖静静刘思远刘瑞华李为全
Owner XINYU PHARM CO LTD
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