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Preparation method of ivermectin

A technology for ivermectin and abamectin, applied in the field of biological drug preparation, can solve the problems of many crystallization times, high cost, low yield and the like, and achieve the effects of high yield, low production cost and simple operation

Active Publication Date: 2016-12-07
NORTH CHINA PHARMA GROUP AINO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the purification technology of ivermectin mainly adopts the method of multiple cooling and cooling crystallization for purification. This method has low purity, many crystallization times, low yield and high cost.

Method used

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  • Preparation method of ivermectin
  • Preparation method of ivermectin
  • Preparation method of ivermectin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] 1) Prepare the crude product of ivermectin: add 500ml of toluene in the hydrogenation kettle, add 150g of high-quality abamectin from the feed port of the hydrogenation kettle, add 1.3g of catalyst under stirring with nitrogen gas, close the feed port of the autoclave, Replace the air in the hydrogenation tank with nitrogen, then replace the nitrogen in the hydrogenation tank with hydrogen, then heat up to 68°C, open the hydrogen valve until the pressure of the reactor rises to 0.5MPa to carry out the hydrogenation reaction, and take a sample for 1 hour. Until the central control is qualified, the reaction time is 1 hour and 45 minutes; put the above-mentioned feed liquid into the catalyst removal kettle, add 2 g of thiourea, keep the water bath at 50-60 ° C, stir for 2 hours under the protection of nitrogen, then cool down to 30 ° C, pump Filter, obtain the crude product 148g of ivermectin;

[0030] 2) Dissolve it with 650ml of ethanol, heat at 70°C, stir until complet...

Embodiment 2

[0038] 1) Prepare the crude product of ivermectin: add 500ml of toluene in the hydrogenation kettle, add 150g of high-quality abamectin from the feed port of the hydrogenation kettle, add 1.3g of catalyst under stirring with nitrogen gas, close the feed port of the autoclave, Replace the air in the hydrogenation tank with nitrogen, then replace the nitrogen in the hydrogenation tank with hydrogen, then heat up to 68°C, open the hydrogen valve until the pressure of the reactor rises to 0.5MPa to carry out the hydrogenation reaction, and take a sample for 1 hour. Until the central control is qualified, the reaction time is 1 hour and 45 minutes; put the above-mentioned feed liquid into the catalyst removal kettle, add 2 g of thiourea, keep the water bath at 50-60 ° C, stir for 2 hours under the protection of nitrogen, then cool down to 30 ° C, pump Filter, obtain the crude product 148g of ivermectin;

[0039] 2) Dissolve it with 650ml of ethanol, heat at 75°C, stir until complet...

Embodiment 3

[0048]What this embodiment studies is the influence of cooling control conditions on the crystallization of ivermectin. Other test conditions are consistent with those in Example 1. The changed test conditions are that the cooling process of the solution adopts a water bath cooling method. After dropping to 35°C, Replace it with cold brine, and cool down to 15°C to end. The test data are shown in Table 3. It can be seen from the table below that the different cooling methods in the crystallization process affect the selectivity of crystallization. Judging from the impurities of No. 1 to No. 6 in the product, the quality of ivermectin crystals obtained by gradient cooling method will be better than that of Crystallization quality obtained by water bath cooling method. Therefore, what the preparation method of the present invention preferably adopts is gradient cooling method.

[0049] table 3

[0050] Items and Indicators

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Abstract

The invention discloses a preparation method of ivermectin. The preparation method comprises the following steps: (1) preparing an ivermectin rough product; (2) dissolving the ivermectin rough product with a solvent, heating, stirring until the ivermectin rough product is completely dissolved, and maintaining the temperature; (3) adding purified water and formamide into a rough product solution, controlling the fed-batch flow velocity, and cooling, so as to obtain a diluent; (4) adding seed crystals into the diluent, and growing the crystals; (5) carrying out cooling crystallization on the diluent until reaching a certain temperature; and (6) carrying out suction filtration, washing and drying, so as to obtain high-purity ivermectin fine powder. The yield of the preparation method reaches above 85%, and a preparation process having the beneficial effects of simple process, stable yield and capability of producing high-purity ivermectin in a large scale is provided.

Description

technical field [0001] The invention specifically relates to a preparation method of ivermectin, which belongs to the field of preparation of biological medicines. Background technique [0002] Ivermectin is a new type of macrolide antibiotic anthelmintic, which has the advantages of high efficiency, broad spectrum and low toxicity. At present, it is widely used as an insecticide and acaricide for humans, animals and plants, so it is one of the biopesticides with great development potential. Its anthelmintic activity is achieved by inhibiting r-aminobutyric acid (GABA) receptors, thereby blocking nerve conduction, and can prevent and control those parasites that have become resistant to common chemicals. [0003] The technology of preparing ivermectin (Ivermectin) in pharmaceutical industry at present mainly is to generate ivermectin by hydrogenation under the effect of Wilson catalyst with Avermectin, also exists simultaneously dihydroabamectin ( H2Bla! H2Blb) and produce...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/08C07H1/00
CPCC07H1/00C07H17/08
Inventor 孙耀华刘书琴王震陈冬周庆娜冯旭川宋维锋逯凯霄李学红任永胜李玉才宋旭肖殷立山王立秋申海建孙炜董玲李永帅张立萍常红
Owner NORTH CHINA PHARMA GROUP AINO
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