Valrubicin, NSC-246131, AD-32, Valtaxin, Valstar
戊柔比星Chemical Name: N-Trifluoroacetyladriamycin-14-valerate; N-Trifluorodoxorubicin-14-valerate; (2S-cis)-2-[[4-(3-Trifluoroacetylamino-2,3,6-trideoxy-alpha-L-lyxo-hexapyranosyl)oxy]-1,2,3,4,6,11-hexahydro-2,5-12-trihydroxy-7-methoxy-6,11-dioxo-2-naphtacenyl]-2-oxoethyl ester valerate
CAS No. 56124-62-0
项目整合开发状态: Launched-1999
项目研究机构: Celltech (Orphan Drug), Pfizer (Originator), Celltech (Marketer), Anthra (Licensee), Paladin (Licensee)
合成路线:The reaction of daunomycin (I) with trifluoroacetic anhydride in chloroform,and boiling the reaction product with methanol gives N-trifluoroacetyldaunomycin (II),which upon treatment with iodine and calcium oxide in THF gives 14-iodo-N-trifluoroacetyldaunomycin (III).Compound (III) treated with sodium valerate (A) in boiling acetone gives the title compound.The final purification is achieved with silicic acid using chloroform-ethanol (100:1) as solvent.
📌 参考资料/链接：
参考文献标题:N-trifluoroacetyladriamycin-14-alkanoates and therapeutic compositions containing same
文献作者:Israel,M.; Modest,E.J.(Sidney Farber Cancer Institute,Inc.)
参考来源:CA 1060003; US 4035566
📄 详细内容
合成路线:The reaction of daunomycin (I) with trifluoroacetic anhydride in chloroform,and boiling the reaction product with methanol gives N-trifluoroacetyldaunomycin (II),which upon treatment with iodine and calcium oxide in THF gives 14-iodo-N-trifluoroacetyldaunomycin (III).Compound (III) treated with sodium valerate (A) in boiling acetone gives the title compound.The final purification is achieved with silicic acid using chloroform-ethanol (100:1) as solvent.
参考文献标题:AD-32
文献作者:Albonico,S.M.
参考来源:Drugs Fut 1980,5(4),171
合成路线:The reaction of daunomycin (I) with trifluoroacetic anhydride in chloroform,and boiling the reaction product with methanol gives N-trifluoroacetyldaunomycin (II),which upon treatment with iodine and calcium oxide in THF gives 14-iodo-N-trifluoroacetyldaunomycin (III).Compound (III) treated with sodium valerate (A) in boiling acetone gives the title compound.The final purification is achieved with silicic acid using chloroform-ethanol (100:1) as solvent.
参考文献标题:N-Trifluoroacetyladriamycin-14-valerate,an analog with greater experimental antitumor avtivity and less toxicity than adriamycin
文献作者:Israel,M.; et al.
参考来源:Cancer Res 1975,351365-68
产品链接: CAS No. 56124-62-0››