CN101337983A - Method for synthesizing ivermectin from avermectin - Google Patents
Method for synthesizing ivermectin from avermectin Download PDFInfo
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- CN101337983A CN101337983A CNA2008100792185A CN200810079218A CN101337983A CN 101337983 A CN101337983 A CN 101337983A CN A2008100792185 A CNA2008100792185 A CN A2008100792185A CN 200810079218 A CN200810079218 A CN 200810079218A CN 101337983 A CN101337983 A CN 101337983A
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- ivermectin
- avermectin
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- avrmectin
- toluene
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Abstract
The invention discloses a method for synthesizing ivermectin from avermectin, which belongs to the field of biological pharmacy. The method for synthesizing ivermectin is characterized in that the avermectin preprocessing step is added before synthesizing ivermectin; and the avermectin preprocessing method is carried out according to the following steps: dissolving avermectin by heating, washing with sodium hydroxide, extracting, concentrating and drying to remove impurities in avermectin. Accordingly, the use amount of a catalyst in the subsequent synthesis process can be effectively reduced to reduce the production cost. The preprocessed avermectin used for synthesizing ivermectin as the raw material can reduce the use amount of the catalyst by 50%, which can reduce the cost of the entire production process by about 15%.
Description
Technical field
The invention belongs to field of biological pharmacy, relate to a kind of method of synthetic ivermectin, specifically a kind of pretreatment process of using the raw material of synthesizing ivermectin from avermectin.
Background technology
Ivermectin is novel wide spectrum, efficient, low toxicity antibiotics antiparasitic, and particularly nematode and arthropods all have and well kill effect to endoparasite and ectoparasite.The technology of the synthetic ivermectin (Ivermcctin) of pharmaceutical industry all is to form with Avrmectin hydrogenation under the effect of Wilson catalyzer at present.Raw materials used Avrmectin is a kind of biological products that got by fermenting process, and itself has impurity raw material, is mainly the ester class, and these impurity can destroy activity of such catalysts in the catalysis building-up process.Therefore, in actual production, manufacturing enterprise must strengthen catalyst consumption and overcome owing to raw material contains the assorted influence that brings.The price of catalyzer rises steadily on the current market, thereby causes production cost to increase greatly, and does not have other technology and catalyzer to substitute, and therefore, reduces the task of top priority that catalyst consumption just becomes manufacturing enterprise.
Summary of the invention
The technical issues that need to address of the present invention provide a kind of method of synthetic ivermectin, by chemical process the raw material Avrmectin are carried out the impurity elimination pre-treatment, thereby effectively reduce catalyst consumption in the follow-up building-up process, realize the purpose that reduces production costs.
For solving the problems of the technologies described above, the technical solution used in the present invention is:
A kind of method with synthesizing ivermectin from avermectin, the method that comprises synthetic ivermectin, increased the pretreatment process to the raw material Avrmectin before synthetic ivermectin, described pretreated method to the raw material Avrmectin is carried out according to poly-order of following step:
1. heating for dissolving: solvent toluene and Avrmectin are added container according to the ratio of 8～10L/kg, be heated to 65～75 ℃, Avrmectin is dissolved fully;
2. washing: with volume is that 0.4～0.6 times of volume of toluene, concentration are that 0.8～1% sodium hydroxide solution adds described container, stirs and be incubated 1～2 hour;
3. extraction: divide the dehydrogenation sodium oxide by extraction, surplus materials is put into thickening equipment;
4. concentrate: the described surplus materials in the thickening equipment is concentrated, slough solvent toluene;
5. dry: with in the thickening equipment through the vacuum-drying 0.8～1.2 hour under 70～80 ℃ temperature of spissated material, promptly get pretreated Avrmectin.
As a further improvement on the present invention:
In the step heating for dissolving 1., the ratio of toluene and Avrmectin is 9～10L/kg, is heated to 68～72 ℃.
During 2. step washed, the concentration of sodium hydroxide solution was 0.9～1%, and volume is 0.45～0.5 times of a volume of toluene, stirs and be incubated 1.5～2 hours.
5. in the drying, drying temperature is 72～78 ℃ to step, vacuum-drying 0.9～1.1 hour.
As optimization scheme of the present invention:
In the step heating for dissolving 1., the ratio of toluene and Avrmectin is 10L/kg, is heated to 70 ℃.
During 2. step washed, the concentration of sodium hydroxide solution was 1%, and volume is 0.5 times of a volume of toluene, stirs and be incubated 2 hours.
5. in the drying, drying temperature is 75 ℃ to step, vacuum-drying 1 hour.
As a kind of improvement of above-mentioned pretreatment process, described toluene can substitute with acetone.
As another improvement of above-mentioned pretreatment process, the also available ethanol of described toluene substitutes.
As the third improvement of above-mentioned pretreatment process, the also available methyl alcohol of described toluene substitutes.
Owing to adopted technique scheme, the obtained technical progress of the present invention is:
Above-mentioned pretreatment process provided by the present invention, with Avrmectin through heating for dissolving → washing → extraction → concentrate → drying, promptly utilize the purpose that realizes impurity elimination in highly basic and the raw material behind the impurities generation chemical reaction, thereby effectively reduce catalyst consumption in the follow-up building-up process, realize the purpose that reduces production costs.Through pretreated Avrmectin, in the process of follow-up synthetic ivermectin, catalyst consumption is only reduced to and is needed 2% by 4% of original Avrmectin amount as raw material, can save 50% catalyst levels, only this just can make the cost savings 15% of whole process of production.
Embodiment
The present invention is described further below in conjunction with specific embodiment.
Embodiment (one)～(six) all carry out according to poly-order of following step:
1. heating for dissolving: the solvent of respective amount and Avrmectin added in the stainless steel cauldron heat, Avrmectin is dissolved fully.Reactor band thermometer stirs with glass or teflon rod.
2. washing: sodium hydroxide solution is added stirring and insulation in the reactor.
3. extraction: divide the dehydrogenation sodium oxide by extraction, surplus materials is put into concentration tank.
4. concentrate: the described surplus materials in the concentration tank is concentrated, slough solvent.
5. dry: with dry under vacuum in the concentration tank through spissated material.
Each embodiment correlation parameter is as follows:
Promptly get pretreated Avrmectin through above-mentioned steps, be used for the raw material of follow-up synthetic ivermectin.
Claims (8)
1, a kind of method with synthesizing ivermectin from avermectin, the method that comprises synthetic ivermectin, it is characterized in that: before synthetic ivermectin, increase pretreatment process, the pretreated method of raw material Avrmectin is carried out according to poly-order of following step the raw material Avrmectin
1. heating for dissolving: solvent toluene and Avrmectin are added container according to the ratio of 8～10L/kg, be heated to 65～75 ℃, Avrmectin is dissolved fully;
2. washing: with volume is that 0.4～0.6 times of volume of toluene, concentration are that 0.8～1% sodium hydroxide solution adds described container, stirs and be incubated 1～2 hour;
3. extraction: divide the dehydrogenation sodium oxide by extraction, surplus materials is put into thickening equipment;
4. concentrate: the described surplus materials in the thickening equipment is concentrated, slough solvent toluene;
5. dry: with in the thickening equipment through the vacuum-drying 0.8～1.2 hour under 70～80 ℃ temperature of spissated material, promptly get pretreated Avrmectin.
2, a kind of method with synthesizing ivermectin from avermectin according to claim 1 is characterized in that: 1. in the heating for dissolving, the ratio of toluene and Avrmectin is 9～10L/kg to step, is heated to 68～72 ℃.
3, a kind of method with synthesizing ivermectin from avermectin according to claim 2, it is characterized in that: the ratio of toluene and Avrmectin is 10L/kg, is heated to 70 ℃.
4, a kind of method according to claim 1 with synthesizing ivermectin from avermectin, it is characterized in that: during 2. step washs, the concentration of sodium hydroxide solution is 0.9～1%, and volume is 0.45～0.55 times of volume of toluene, stirs and be incubated 1.5～2 hours.
5, a kind of method according to claim 4 with synthesizing ivermectin from avermectin, it is characterized in that: the concentration of sodium hydroxide solution is 1%, volume is 0.5 times of a volume of toluene, stirs and be incubated 2 hours.
6, a kind of method with synthesizing ivermectin from avermectin according to claim 1 is characterized in that: 5. in the drying, drying temperature is 72～78 ℃ to step, vacuum-drying 0.9～1.1 hour.
7, the synthetic ivermectin according to claim 6 pretreatment process of Avrmectin, it is characterized in that: drying temperature is 75 ℃, the vacuum-drying time is 1 hour.
8, a kind of method with synthesizing ivermectin from avermectin according to claim 1, it is characterized in that: described toluene substitutes with the wherein a kind of of acetone, ethanol or methyl alcohol.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100792185A CN101337983A (en) | 2008-08-20 | 2008-08-20 | Method for synthesizing ivermectin from avermectin |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100792185A CN101337983A (en) | 2008-08-20 | 2008-08-20 | Method for synthesizing ivermectin from avermectin |
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| Publication Number | Publication Date |
|---|---|
| CN101337983A true CN101337983A (en) | 2009-01-07 |
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| Application Number | Title | Priority Date | Filing Date |
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| CNA2008100792185A Pending CN101337983A (en) | 2008-08-20 | 2008-08-20 | Method for synthesizing ivermectin from avermectin |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103396464A (en) * | 2013-07-16 | 2013-11-20 | 河北威远动物药业有限公司 | Preparation method of ivermectin |
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2008
- 2008-08-20 CN CNA2008100792185A patent/CN101337983A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103396464A (en) * | 2013-07-16 | 2013-11-20 | 河北威远动物药业有限公司 | Preparation method of ivermectin |
| CN103396464B (en) * | 2013-07-16 | 2017-04-05 | 河北威远动物药业有限公司 | A kind of preparation method of ivermectin |
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Open date: 20090107 |