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The method of extraction of artemisinin Artemisinin

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Updated: Tuesday, Oct 06,2015, 9:26:35 AM
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The extraction method of artemisinin from Artemisia annua by extraction principle as the foundation, mainly with ether extraction and solvent extraction of gasoline. The essential oil was extracted by steam distillation, vacuum distillation separation, the process was: feeding, water, distilled water, oil and water separation, non volatile components mainly used organic solvent extraction, column chromatography and recrystallization separation, the basic process is: drying, crushing, extraction (repeated) - concentrated extract, crude oil - refining.

Chemical synthesis

Semi synthetic route: starting from artemisinic acid as raw material, after five step reaction of artemisinin, total rate of about 35 ~ 50%.

The first step: artemisinic acid in diazomethane / iodine methane / acid catalyzed reaction with methanol, in nickel chloride in the presence of conditions, a reduction of sodium borohydride selectively dihydroartemisinic acid methyl ester;

The second step: two hydrogen artemisinic acid methyl ester with lithium aluminum hydride reduction artenimol in tetrahydrofuran or ether solution;

The third step: artenimol in methanol / dichloromethane / chloroform / carbon tetrachloride solution by ozone oxidation get peroxide, drained and in xylene with of toluene sulfonic acid treatment to obtain cyclic enol ether;

The fourth step: cyclic enol ether dissolved in the solvent, the photosensitizer Rose Bengal / methylene blue / hypocrellin et presence through photo oxidation and produce oxygen tetracyclic intermediate and then acid treatment by decarboxylation of artemisinin.

The fifth step: the decarboxylation of artemisinin in four ruthenium oxide oxidation system or chromate oxidants under the effect of oxidation of artemisinin.

Synthetic route: it can be synthesized by a variety of routes. Such as Schmil 1983 reported a application of key compounds enol ether at low temperature light oxidation reaction to introduce peroxy radical total synthesis reaction to (-) - 2 - isomenthol as raw material, keep raw materials in the six membered ring, ring three side chain alkylation, the formation of intermediates, the posterior ring synthesized with peroxide Bridge times sesquiterpene lactone. Xing Xiang Xu equal to 1986 reported the chemical synthesis of artemisinin pathway and the synthesis to R - (+) - vanillin as raw material, after 14 - step synthetic artemisinin.

Biosynthesis

The biosynthesis of artemisinin and other times and the like in the cytoplasm, the pathway of the plant type of the metabolic pathway, can be divided into three steps: the formation of FPP by acetic acid, the synthesis of the times of the semi -, and then the formation of artemisinin. : FPP - 4,11- diene sesquiterpene, artemisinic acid, two hydrogen, two oxygen artemisinic acid peroxide, artemisinin and artemisinic acid. In the bud of Artemisia annua, hairy root cultures of Artemisia annua L. Agrobacterium rhizogenes and training system of artemisinin synthesis technology is likely to be applied to industrial production.

Tags: Arteannuin、-Artemisi

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