Artemisinin synthetic method

Abstract

The invention relates to an artemisinin synthetic method. The method comprises the following steps: 1) taking arteannuic acid as a raw material, and generating dihydroartemisinic acid through a reduction reaction, wherein the reduction reaction is carried out on arteannuic acid under existence of a reaction solvent; 2) obtaining a dihydroartemisinic acid derivative under protection of carboxyl group by dihydroartemisinic acid, wherein carboxyl group protection is characterized in that under alkalescence existence, dihydroartemisinic acid is subjected to carboxyl group protection in an organicsolvent to obtain the dihydroartemisinic acid derivative, wherein mol ratio of the dihydroartemisinic acid to alkali is 1:(1-30), reaction temperature is 50-60 DEG C, and the used alkali can be inorganic base or organic base for the reaction; 3) performing an oxidation reaction on the dihydroartemisinic acid derivative to obtain the corresponding peroxy dihydroartemisinic acid derivative; and 4) performing rearrangement on the peroxy dihydroartemisinic acid derivative under acid catalysis, and performing repurification to obtain the artemisinin. The synthetic method has the advantages of simple technology, high purification efficiency, and low preparation cost.

Description

technical field [0001] The invention belongs to the field of artemisinin preparation technology, and in particular relates to a synthesis method of artemisinin. Background technique [0002] Artemisinin is a colorless needle-like crystal extracted from the leaves of the compound inflorescence plant Artemisia annua, which is the traditional Chinese medicine Artemisia annua. Its stem does not contain the drug Artemisia annua. The most effective antimalarial drugs after that, especially for cerebral malaria and anti-chloroquine malaria, have the characteristics of quick action and low toxicity, and were once called "the only effective malaria treatment drug in the world" by the World Health Organization; antimalarial effect The mechanism mainly lies in the generation of free radicals through the activation of artemisinin during the treatment of malaria. The free radicals combine with malaria protein and act on the membrane structure of Plasmodium, destroying the vesicular membr...

AI Technical Summary

Problems solved by technology

[0002] Artemisinin is a colorless needle-like crystal extracted from the leaves of the compound inflorescence plant Artemisia annua, which is the traditional Chinese medicine Artemisia annua. Its stem does not contain the drug Artemisia annua. The most effective antimalarial drugs after that, especially for cerebral malaria and anti-chloroquine malaria, have the characteristics of quick action and low toxicity, and were once called "the only effective malaria treatment drug in the world" by the World Health Organization; antimalarial effect The mechanism mainly lies in the generation of free radicals through the activation of artemisinin during the treatment of malaria. The free radicals combine with malaria protein and act on the membrane structure of Plasmodium, destroying the vesicular membrane, nuclear membrane and plasma membrane, and the mitochondria Swelling, inner and outer membranes fall off, thereby destroying the cell structure and function of Plasmodium; in addition, artemisinin also shows attractive prospects in the treatment of other diseases; such as anti-schistosomiasis, regulating or inhibiting the immune function of humoral, improving The conversion rate of lymphocytes, choleretic, expectorant, antitussive, asthma, etc., so artemisinin has great medical market prospects; the current synthesis method of artemisinin has low efficiency and cannot meet the needs of rapid synthesis , so it is necessary to improve the extraction and separation method of artemisinin