Pu Y M, Torok D S, Ziffer H, Pan X Q, Meshnick S R
Laboratory of Chemical Physics, NIDDK, Bethesda, Maryland 20892-0510, USA.
J Med Chem. 1995 Sep 29;38(20):4120-4. doi: 10.1021/jm00020a028.
The carbonyl groups in several artemisinin derivatives were converted into geminal difluorinated compounds on treatment with diethylaminosulfur trifluoride. A number of other mono- and polyfluorinated artemisinin derivatives were prepared. Their in vitro antimalarial activities were all equal to or greater than the nonfluorinated analogs or precursors.
几种青蒿素衍生物中的羰基在与二乙氨基三氟化硫反应时被转化为偕二氟代化合物。制备了许多其他单氟和多氟青蒿素衍生物。它们的体外抗疟活性均等于或高于未氟化的类似物或前体。
