71963-77-4Relevant articles and documents
One-pot green synthesis of β-artemether/arteether
Kumar, Atul,Bishnoi, Ajay Kumar
, p. 31973 - 31976 (2014)
An efficient one pot green synthesis of β-artemether/arteether from artemisinin has been developed using a sodium borohydride-cellulose sulfuric acid (CellSA) catalyst system. The green methodology is high yielding and the catalyst has good recyclability.
A process for preparing β - pedic ether process
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Paragraph 0023-0024; 0025-0026; 0027-0028, (2018/04/21)
The invention discloses a technology for preparing beta-artemether. The technology comprises the following steps: reducing an initial raw material artemisinin in the presence of a reducing agent to generate dihydroartemisinin, and carrying out an etherification reaction on dihydroartemisinin and trimethyl orthoacetate in the presence of a catalyst to prepare beta-artemether. Experiments prove that the technology allows the content of alpha-artemether generated in the methyl etherification reaction to be smaller than 3%, the HPLC purity of the obtained beta-artemether to be improved to above 99.8%, the content of single impurities to be smaller than 0.1% respectively and the quality of the above product to accord with requirements of United States Pharmacopeia; and the total mole yield of the product by artemisinin can reach 95% or above. The technology can avoid tedious intermediate processing links in the prior art, realizes simple-operation low-cost high-yield preparation of highly pure beta-artemether, accords with industrial production demands of beta-artemether, and has industrial application values.
Method for producing artesunate
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Paragraph 0012-0036, (2017/06/06)
The invention relates to a method for producing artesunate. The method is characterized by comprising the following steps: (a) carrying out a reaction: adding dihydroartemisinin into dichloromethane, then, adding methanol and perchloric acid, carrying out the reaction for 10 to 15 minutes, adding anhydrous sodium carbonate to terminate the reaction, and filtering the reaction solution; (b) carrying out concentration: concentrating the filtered reaction solution in a water bath with the temperature of about 55 DEG C; (d) carrying out crystallization: subjecting the concentrated mother liquor to freeze-crystallizing, and carrying out centrifugal filtration, so as to obtain crude crystals; (e) carrying out refining: dissolving the crude crystals with methanol at the temperature of 65 DEG C so as to obtain a saturated solution, carrying out cooling-crystallization, and carrying out centrifugal filtration; and (f) carrying out baking: subjecting the crystals to vacuum drying for 120 minutes at the temperature of 55 DEG C, thereby obtaining a finished product. According to the method, the yield can reach 76% in case of not treating the generated mother liquor, the reaction time is short, energy is saved, and the production cost is reduced.