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71963-77-4 Dihydroartemisin methyl ether Keywords antimalarial drugs
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According to WHO intravenous AS is the drug of choice for severe malaria both in children and adults where there is low transmission.In regions where transmission is high, randomized trials among Asian adults and African children strongly advocates the use of artesunate over quinine as the treatment of choice for falciparum malaria.
Artesunate is prepared from dihydroartemisinin (DHA) by reacting it with succinic acid anhydride in basic medium. Pyridine as base/solvent, sodium bicarbonate in chloroform and catalyst DMAP (N,N-dimethylaminopyridine) and triethylamine in 1,2-dichloroethane have been used, with yields of up to 100%. A large scale process involves treatment of DHA in dichloromethane with a mixture of pyridine, a catalytic amount of DMAP and succinic anhydride. The dichloromethane mixture is stirred for 6–9 h to get artesunate in quantitative yield. The product is further re-crystallized from dichloromethane. alpha-Artesunate is exclusively formed (m.p 135–137C).
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