【药物名称】Valrubicin, NSC-246131, AD-32, Valtaxin, Valstar
化学结构式(Chemical Structure):
参考文献No.46986
标题:N-trifluoroacetyladriamycin-14-alkanoates and therapeutic compositions containing same
作者:Israel, M.; Modest, E.J. (Sidney Farber Cancer Institute, Inc.)
来源:CA 1060003; US 4035566
合成路线图解说明:

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No.65178
标题:AD-32
作者:Albonico, S.M.
来源:Drugs Fut 1980,5(4),171
合成路线图解说明:

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No.800224
标题:N-Trifluoroacetyladriamycin-14-valerate, an analog with greater experimental antitumor avtivity and less toxicity than adriamycin
作者:Israel, M.; et al.
来源:Cancer Res 1975,351365-68
合成路线图解说明:

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.

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