The Synthesis Process Of Artemether And Analysis

Artemisinin was first isolated from Herba artemisiae annuae by Chinese scientists in 1972. It is an effective antimalarial drug against chloroquine-resistant Plasmodium falciparum strains and cerebral malaria with low toxicity. In order to develop more potent, better water-soluble, less neurotoxic agents, a large mount of artemisinin analogs have been synthesized by the side chain changing or structure simplifying. As ARM is the representational one among them, it possesses convenient for making the preparations besides the above merits. And it is considered as the front-line antimalariarial drug by WHO.On the basis of reference to the research of ARM, the method of two-step process for the synthesis of ARM was chosen to prepare the product after the pre-experiments. DHA was got by the redox to Artemisinine and changed to the target product, ART after etherification reaction. Each of the synthetic conditions which influence the yields for DHA and ARM was discussed in details in this article. The results showed that the dominant factors for synthesis of ART were the dose of dichloroethene, the amount of catalyst, the temperature of the reaction, and the reaction time. So the synthetic process was then optimized by the method of orthogonal design for the purpose to enhance the yield of ARM. The yield rate attains 71.0% for DHA and 69.9% respectively.In additional, an HPLC method without derivation reactions to determine the content of ART, DHA and ARM was built and its suitabilities for the derivatives was studied. Especially, the method for determining ARM, DHA directly was put forward at the peak of 210nm. It was proved to be more accurate and convenient which supply a more dependable means to evaluate the exact content for ARM drugs.The structure characteristic testing shows that the structure of the synthetic compound is absolutely consistent with ARM. The content and purity of the sample are both reaching the quality standard of the National medicines and drugs.