(-)-C-demethyl arteannuin B is a structural analog of the antimalarial artemisinin. It exhibits potent antimalarial activity even against a drug-resistant strain. Little and coworkers obtained the alkylated hydrazone in diastereomerically pure form (de > 95%) through the Enders' alkylation reaction. This intermediate was then elaborated into (-)-C-demethyl arteannuin B.