[摘要]：An efficient conversion of artemisinin into three new amino- and hydroxy-functionalized 11-aza prototypes I (X = NH2, OH, HOCH2CH2) has been achieved on a multigram scale by reaction with hydrazine, hydroxylamine, and 2-aminoethanol, resp. I (X = NH2) was further diversified by N-acylation with aroyl chlorides and diacyl dichlorides and imination/reductive amination with arom. aldehydes. I (X = OH, HOCH2CH2) were converted into the corresponding ethers on treatment with alkyl bromides in the presence of NaH. Some of these compds. showed a high order of activity against multidrug-resistant malaria in mice by oral route.
