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新产品编号:1747037

Chemical Name: (3R,5aS,6R,8aS,9R,10R,12R,12aR)-10-[2-(2-Fluorobenzyloxy)ethyl]-3,6,9-trimethylperhydro-3,12-epoxypyrano[4,3-j]-1,2-benzodioxepine; 10beta-[2-(2-Fluorobenzyloxy)ethyl]-10-deoxoartemisinin
项目整合开发状态: Preclinical
项目研究机构: University of Liverpool (Originator)
合成路线:Coupling of dihydroartemisinin (I) with allyl trimethylsilane in the presence of boron trifluoride etherate gave the 10beta-allyl deoxo derivative (II).Subsequent ozonization of the allyl double bond of (II),followed by reductive treatment with NaBH4,provided alcohol (III).Finally,alkylation of (III) with 2-fluorobenzyl bromide (IV) in the presence of NaH furnished the corresponding 2-fluorobenzyl ether.
📌 参考资料/链接:
参考文献标题:Novel,potent,semisynthetic antimalarial carba analogues of the first-generation 1,2,4-trioxane artemether
文献作者:O'Neill,P.M.; Searle,N.L.; Kan,K.W.; Storr,R.C.; Maggs,J.L.; Ward,S.A.; Raynes,K.; Park,K.
参考来源:J Med Chem 1999,42(26),5487