新产品编号:683933
Chemical Name: (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
CAS No. 256341-25-0
项目整合开发状态: Preclinical
项目研究机构: Johns Hopkins University (Originator), Ultrafine (Originator), University of Liverpool (Originator)
合成路线: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.
📌 参考资料/链接：
参考文献标题:Peroxide-based antimalarial cpds.
文献作者:Ward,S.A.; O'Neill,P.M.(Ultrafine Ltd.)
参考来源:WO 0104123
📄 详细内容
合成路线: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.
参考文献标题:Synthesis,antimalarial activity,biomimetic iron(I) chemistry,and in vivo metabolism of novel,potent C-10-phenoxy derivatives of dihydroartemisinin
文献作者:O'Neill,P.M.; Miller,A.; Bishop,L.P.D.; Hindley,S.; Maggs,J.L.; Ward,S.A.; Roberts,S.M.; Scheinmann,F.; Stachulski,A.V.; Posner,G.H.; Park,B.K.
参考来源:J Med Chem 2001,44(1),58
合成路线: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.
参考文献标题:Application of the TMSOTf-AgClO4 activator system to the synthesis of novel,potent,C-10 phenoxy derivatives of dihydroartemisinin
文献作者:O'Neill,P.M.; et al.
参考来源:Tetrahedron Lett 1999,40(51),9129