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【结 构 式】 
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【药物名称】 【化学名称】(3R,5aS,6R,8aS,9R,10S,12R,12aR)-3,6,9-Trimethyl-10-[4-(trifluoromethyl)phenoxy]decahydro-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin 【CA登记号】256341-25-0 【 分 子 式 】C22H27F3O5 【 分 子 量 】428.45269 |
【开发单位】Johns Hopkins University (Originator), Ultrafine (Originator), University of Liverpool (Originator) 【药理作用】ANTIINFECTIVE THERAPY, Antimalarials, Treatment of Protozoal Diseases |
合成路线1
Coupling of dihydroartemisinin (I) with p-trifluoromethylphenol (II) in the presence of trimethylsilyl triflate and silver perchlorate at -78 C produced the corresponding aryl ether as an epimeric mixture. The major 10-beta isomer was then isolated from the reaction mixture by column chromatography.
| 【1】 O'Neill, P.M.; et al.; Application of the TMSOTf-AgClO4 activator system to the synthesis of novel, potent, C-10 phenoxy derivatives of dihydroartemisinin. Tetrahedron Lett 1999, 40, 51, 9129. |
| 【2】 O'Neill, P.M.; Miller, A.; Bishop, L.P.D.; et al.; Synthesis, antimalarial activity, biomimetic iron(I) chemistry, and in vivo metabolism of novel, potent C-10-phenoxy derivatives of dihydroartemisinin. J Med Chem 2001, 44, 1, 58. |
| 【3】 Ward, S.A.; O'Neill, P.M. (Ultrafine Ltd.); Peroxide-based antimalarial cpds.. WO 0104123 . |
Extended Information