Artemether

854

IHS/IP/INP

Antimalarial

TP (Technical Package)

[71963-77-4]

[3 R- (3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,12a R* )]-Decahydro-10-methoxy-3 ,6,9-trimethyl-3,12-epoxy-12 H- p yrano[4,3- j ]-1,2-benzodioxepin

dihydroartemisinin methyl ether; dihydroqinghaosu methyl ether; o- methyldi hydroartemisinin

Paluther (RPR)

SM-224

C 16 H 26 O 5

298.38

C 64.41%, H 8.78%, O 26.81% .

Derivative of arte misinin, q.v. Prepn: Y. Li et al., K prime o Hseuh T prime ung Pao 24, 667 (1979), C.A. 91, 211376u (1979); eidem, Acta Pharm. Sinica 16, 429 (1981). Absolute configuration: X.-D. Luo et al., Helv. Chim Acta 67, 1515 (1984). NMR spectral study: F. S. El-Feraly et al., Spectrosc. Lett. 18, 843 (1985). Inhibition of protein synthesis: H. M. Gu et al., Biochem. Pharmacol. 32, 2463 (1983). Antimalarial activity: S. Thai thong, G. H. Beale, Bull. WHO 63, 617 (1985). Series of articles on chemistry, pharmacology and antimalar ial effi cacy: China Cooperative Research Group on Qinghaosu, J. Tradit. Chinese Med. 2, 3-50 (1982). Toxicity data:  eidem, ibid. 31. Clinical trial in cerebral malaria in children: M. B. van Hensbroek et al., N. Engl. J. Med. 335, 69 (1996)

Crystals, mp 86-88degrees. [Alpha] D 19.5 171degrees (c = 2.59 in CHCl 3) . LD 50 i.m. in mice: 263 mg/kg (China Cooperative Research Group on Qinghaosu)

86-88

171