The Design And Synthesis Of Water-soluble Prodrug Of Dihydroartemisnin

Objective: The design and synthesis of water-soluble prodrug of Dihydroartemisinin;Methods: Dihydroartemisinin was etherified with 4-acetoxybenzyl alcohol as the Presence of boron trifluoride,then de-protection under alkaline condition,and then reacted with 4-methyl-piperazine-1-carbonyl chloride catalysted by 4-ppy to get the target product;Results: The target product was identified by mass spectrum and H1-NMR.Conclusion: The target compound showed a good water-solubility and the rabbit metabolism experiment showed a good result that the Metabolites of CQMU-DHA-10 contains Dihydroartemisinin.