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Method and equipment for scale production of artemisinin

A large-scale technology for artemisinin, which is applied in the field of large-scale preparation of artemisinin, can solve the problems of complex operation and long reaction time, and achieve the effects of low exothermic effect, low manufacturing cost and improved utilization rate

Active Publication Date: 2014-04-23
HUNAN KEYUAN BIO PRODS
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  • Abstract
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Problems solved by technology

[0013] CN 103172645 A discloses a high-efficiency synthesis method of pennyroycin, comprising the following steps: obtaining dihydrocyanine through the protection of shuttle group Pennylic acid derivatives, which are oxidized by peroxides in the presence of catalysts to corresponding dihydroperoxidic pennylic acid derivatives, and then under the catalysis of acids and the action of oxygen, the target product pennyringin can be obtained in high yields, The yield of this method is about 60%, but the reaction time is long and the operation is complicated

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  • Method and equipment for scale production of artemisinin
  • Method and equipment for scale production of artemisinin

Examples

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Embodiment 1

[0044] The photosensitive oxidation reaction equipment consists of a constant temperature tank 1 and ten 6L photoreactors 2. The photoreactors 2 are fixed in the constant temperature tank 1, and the light sources 2-3 used are LED light sources.

[0045] Dissolve 6Kg of dihydroartemisinic acid in 50 liters of toluene, add 2Kg of trifluoroacetic acid and 20g of tetraphenylporphyrin to it, and stir evenly; equal parts are divided into 10 parts, and added to 10 photoreactors 2 respectively ;Adjust the temperature of thermostat 1 to -30 o C. After half an hour of passing oxygen through the interface 2-6 at the bottom of the chromatography column 2-1, turn on the light source 2-3, and the reaction system is at -30 o C to react for 4 hours; then, slowly raise the reaction system to 25°C, react for another 1 hour, turn off oxygen and light source 2-3; pour the reaction solution from the reactor, and adjust the reaction system with saturated aqueous sodium bicarbonate solution To weak...

Embodiment 2

[0047] The photosensitive oxidation reaction equipment consists of a constant temperature tank 1 and twenty 6L photoreactors 2, the photoreactors 2 are fixed in the constant temperature tank 1, and the light sources 2-3 used are LED light sources.

[0048] Dissolve 10Kg of dihydroartemisinic acid in 100 liters of toluene, add 3.5Kg of trifluoroacetic acid and 35g of tetraphenylporphyrin to it, stir evenly; divide the same amount into 20 parts, and add them to 20 photoreactors in turn ;Adjust the temperature of thermostat 1 to -50 o C. After half an hour of passing oxygen through the interface 2-6 at the bottom of the chromatography column 2-1, turn on the light source 2-3, and the reaction system is at -50 o C to react for 4 hours; then, slowly raise the reaction system to 20°C, react for another 1 hour, turn off the oxygen and the light source 2-3; pour the reaction solution from the reactor, and adjust the reaction system with saturated aqueous sodium bicarbonate solution T...

Embodiment 3

[0050] The photosensitive oxidation reaction equipment consists of a constant temperature tank 1 and 20 10L photoreactors 2, the photoreactors 2 are fixed in the constant temperature tank 1, and the light sources 2-3 used are LED light sources.

[0051]Dissolve 15Kg of dihydroartemisinic acid in 150 liters of toluene, add 5Kg of trifluoroacetic acid and 60g of tetraphenylporphyrin to it, and stir evenly; equally divide into 20 parts, and add them to 20 photoreactors in turn; Adjust the temperature of constant temperature tank 1 to -20 o C. After half an hour of passing oxygen through the interface 2-6 at the bottom of the chromatography column 2-1, turn on the light source 2-3, and the reaction system is at -20 o C reaction for 4 hours; then, slowly raise the reaction system to 25°C, react for another 1 hour, turn off the oxygen and light source 2-3; pour the reaction solution from the reactor, and adjust the reaction system with saturated aqueous sodium bicarbonate solution ...

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Abstract

The invention relates to a method and equipment for scale production of artemisinin. The method comprises: dissolving dihydroarteannuic acid in an organic solvent, adding a photosensitizer and an acid catalyst, adopting a light source to make the dihydroarteannuic acid be subjected to light oxidation so as to obtain peroxy alcohol of the dihydroarteannuic acid, carrying out acid catalysis so as to carry out Hock cut-off, and carrying out oxidation ring closing to produce the artemisinin, wherein the whole reaction or only the light oxidation reaction is performed in photosensitive oxidation reaction equipment. The present invention further comprises the photosensitive oxidation reaction equipment for performing the method. According to the present invention, the method has characteristics of low reaction temperature and high light source utilization rate, and the equipment has characteristics of high light source utilization rate, simple structure, low manufacturing cost, and high single-batch productivity.

Description

technical field [0001] The invention relates to a preparation method and equipment for artemisinin, in particular to a method and equipment for large-scale preparation of artemisinin. Background technique [0002] Artemisinin and its derivatives are currently the most effective antimalarial drugs with low toxicity, and are the first natural medicines recognized internationally. [0003] Artemisinin is a compound containing peroxy-sesquiterpene lactones. Its antimalarial effect is through interfering with the membrane-mitochondrion function of Plasmodium, which leads to the complete disintegration of the parasite structure. Some derivatives of artemisinin, such as dihydroartemisinin and artemether, have higher antimalarial efficacy. [0004] At present, artemisinin is mainly extracted from the Chinese herbal medicine Artemisia annua (Artemisia annua). The global raw materials of Artemisia annua mainly come from Youyang, Chongqing, China, and the production of Artemisia annu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D493/20B01J19/12
CPCB01J19/122C07D493/20
Inventor 林文彬刘志强
Owner HUNAN KEYUAN BIO PRODS
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