新产品编号:600087
Chemical Name: 1,1'-(1,4-Phenylene)bis[2-[(3R,5aS,6R,8aS,9R,10R,12R,12aR)-3,6,9-trimethyl-3,12-epoxyperhydropyrano[4,3-j]-1,2-benzodioxepin-10-yl]ethanone]
CAS No. 229981-82-2
项目整合开发状态: Preclinical
项目研究机构: Hauser (Originator), Johns Hopkins University (Originator)
合成路线:Reduction of artemisinin (I) by means of NaBH4 in THF/MeOH followed by treatment with BH3稨2O in MeOH yields (II).Finally,beta-artemether (II) is condensed with TMS-enol ether (IV) [obtained by protection of diacetylbenzene (III) by means of TMSOTf and Et3N in THF] in the presence of TiCl4 in CH2Cl2.
📌 参考资料/链接：
参考文献标题:C-10 carbon-substd.artemisinin-like trioxane cpds.having antimalarial,antiproliferative and antitumour activities
文献作者:Parker,M.H.; Shapiro,T.A.; Ploypradith,P.; Posner,G.H.; Northrup,J.; Daughenbaugh,R.J.; Woo,S.H.; Murray,C.; Elias,J.S.; Zheng,Q.Y.(Hauser,Inc.; Johns Hopkins University)
参考来源:EP 1043988; WO 9933461
📄 详细内容
合成路线:Reduction of artemisinin (I) by means of NaBH4 in THF/MeOH followed by treatment with BH3稨2O in MeOH yields (II).Finally,beta-artemether (II) is condensed with TMS-enol ether (IV) [obtained by protection of diacetylbenzene (III) by means of TMSOTf and Et3N in THF] in the presence of TiCl4 in CH2Cl2.
参考文献标题:Antimalarial,antiproliferative,and antitumor activities of artemisinin-derived,chemically robust,trioxane dimers
文献作者:Posner,G.H.; Ploypradith,P.; Parker,M.H.; O'Dowd,H.; Woo,S.H.; Northrop,J.; Krasavin,M.; Dolan,P.; Kensler,T.W.; Xie,S.; Shapiro,T.A.
参考来源:J Med Chem 1999,42(21),4275