The total synthesisofd ehydroantofine was achieved by employing an ovel, regioselective, azahetero Diels-Alder reaction of easilya ccessible 3,5-dichloro-2H-1,4-oxazin-2-one with 14 a as ak ey step. Furthermore, it is demonstrated that dehydroantofinei sapromisingc andidate as an ew antimalarial agent in ab iological assay with chloroquine-resistant Plasmodium falciparum.
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