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Method and equipment for preparing artemisinin by adopting dihydroarteannuic acid as raw material

A technology of dihydroartemisinic acid and artemisinin, applied in chemical instruments and methods, chemical/physical/physicochemical processes of energy application, chemical/physical/physicochemical processes, etc., can solve complicated operation and long reaction time and other problems, to achieve the effect of reducing the reaction temperature, low production cost and reasonable design

Active Publication Date: 2014-04-23
HUNAN KEYUAN BIO PRODS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 preparing artemisinin by adopting dihydroarteannuic acid as raw material
  • Method and equipment for preparing artemisinin by adopting dihydroarteannuic acid as raw material

Examples

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Effect test

Embodiment 1

[0041] The dihydroartemisinic acid of 200g is dissolved in the dichloromethane of 1000mL, then pours in the photoreactor, then adds trifluoroacetic acid 80g and photosensitizer tetraphenylporphyrin 1g in the reactor; Reaction system is cooled to At -20°C, oxygen was introduced from the bottom port of the reactor through the sand core at a flow rate of 3L / min; half an hour later, the high-pressure mercury lamp was switched on, and the light reaction was carried out continuously for 4 hours at -20°C; then, the reaction system was The temperature was slowly raised to 20°C, stirred for 1 hour, and the light source was turned off.

[0042] Pour out the reaction solution, wash twice with 100 mL of saturated sodium bicarbonate solution, wash the organic phase with 50 mL of water, dry over anhydrous sodium sulfate, filter, and concentrate to obtain a crude product; the crude product is reconstituted with a mixed solvent of ethanol and petroleum ether Crystallized to obtain 145g of art...

Embodiment 2

[0045] Dissolve 100g of dihydroartemisinic acid in 500mL of dichloromethane, then pour it into the photoreactor, then add 1g of photosensitizer rose bengal to the reactor, cool the reaction system to -50°C, Oxygen was introduced into the bottom interface through the sand core at a flow rate of 3L / min; after half an hour, the medium-pressure mercury lamp was switched on, and the light reaction was continued for 4 hours at -50°C; the light source was turned off, and then 40g of tris Fluoroacetic acid, and then continue to feed oxygen for 1 hour; then, slowly raise the temperature of the reaction system to 25° C., and react for 1 hour.

[0046] Pour out the reaction solution, wash twice with 50 mL of saturated sodium bicarbonate solution, then wash the organic phase with 30 mL of water, dry over anhydrous sodium sulfate, filter, and concentrate to obtain a crude product; use a mixed solvent of ethanol and petroleum ether for the crude product Recrystallized to obtain 73g of artem...

Embodiment 3

[0048]Dissolve 200g of dihydroartemisinic acid in 1000mL of dichloromethane, then pour it into the photoreactor, and then add 1g of photosensitizer tetraphenylporphyrin to the reactor; cool the reaction system to -10°C, from the reaction Oxygen was introduced into the bottom of the device through the sand core at a flow rate of 3L / min; half an hour later, the deuterium lamp was switched on, and the light was continuously illuminated at -10°C for four hours.

[0049] Turn off the light source, pour out the reaction solution, quickly transfer it to a 2L three-neck flask, stir, and cool down to -20°C, feed oxygen at a flow rate of 3L / min, slowly add 80g of trifluoroacetic acid to the reaction system, and The reaction was carried out at 20° C. for 2 hours, and then the temperature of the reaction system was slowly raised to 25° C. and stirred for 1 hour.

[0050] Pour out the reaction solution, wash twice with 100 mL of saturated sodium bicarbonate solution, then wash the organic ...

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Abstract

The invention relates to a method and equipment for preparing artemisinin by adopting dihydroarteannuic acid as a raw material. 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 the photoreactor. The present invention further comprises the photoreactor for performing the method. According to the present invention, the method has characteristics of low reaction temperature, high artemisinin yield and high light source utilization rate, and the equipment has characteristics of simple structure, low manufacturing cost, and high single-batch productivity.

Description

technical field [0001] The invention relates to a method and equipment for preparing artemisinin, in particular to a method and equipment for preparing artemisinin with dihydroartemisinic acid as a raw material. Background technique [0002] Artemisinin and its derivatives are currently the most effective and low-toxic antimalarial drugs, and are the first internationally recognized natural medicines today. [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 th...

Claims

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Application Information

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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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