MHP-46

Chemical Name: (3R,5aS,6R,8aS,9R,10R,12S,12aR)-Octahydro-3,6,9-trimethyl-10-(2-furyl)-3,12-epoxy-12H-pyrano[4,3-j][1,2]benzodioxepin
CAS No. 204503-68-4
项目整合开发状态: Biological Testing
项目研究机构: Johns Hopkins University (Originator)
合成路线:Artemisinin (I) was reduced to the dihydro analogue (II),and subsequently the 10-hydroxyl group was substituted for a fluorine atom using diethylaminosulfur trifluoride.The desired 10-beta-isomer (III) was then separated by column chromatography.Finally,boron trifluoride-promoted Friedel Crafts condensation with furan (IV) at low temperature provided the target furyl compound,the major 10-beta isomer being isolated by chromatography on Florisil.
📌 参考资料/链接:
参考文献标题:Orally active,hydrolytically stable,semisynthetic,antimalarial trioxanes in the artemisinin family
文献作者:Posner,G.H.; Parker,M.H.; Northrop,J.; Elias,J.S.; Ploypradith,P.; Xie,S.; Shapiro,T.A.
参考来源:J Med Chem 1999,42(2),300