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CN101289468A 一种新型的奥沙利铂衍生物 无效 - 撤回

一种新型的奥沙利铂衍生物
摘要：
本发明涉及一种新型的奥沙利铂衍生物[1R，2R－环己烷二胺·2，2－二(羟甲基)－1，3－丙二酸根合铂(II)]，[(1R，2R－cyclohexanediamine)·2，2－Bis(hydroxymethyl)malonato－platinum(II)]。它的制备是以cis－[PtA2I2]为原料(A2＝1R，2R－环己烷二胺)，与2，2－二(羟甲基)－1，3－丙二酸银定量反应，过滤分离AgI后母液浓缩和冷冻干燥得到粗品，粗品经水∶乙醇＝1∶1的体系中重结晶得到纯品。本发明配合物的抗癌活性明显高于奥沙利铂、毒副作用明显比奥沙利铂小，可以制成冻干粉或注射液，用于临床治疗癌症。
摘要（英）：

The invention relates to a novel oxaliplatin derivative of (1R, 2R-cyclohexanediamine.2, 2-Bis (hydroxymethyl)-1, 3-malonato-platinum (II)) and ((1R, 2R-cyclohexanediamine).2, 2-Bis (hydroxymethyl)malonato-platinum (II)). The derivative is prepared with the steps that the cis-(PtA2I2) (A2 is equal to 1R, 2R-cyclohexanediamine) is adopted as the raw material and quantitatively reacts with the 2, 2-Bis (hydroxymethyl)-1, 3-malonate silver, and a crude product then is obtained through the mother liquor concentration and freeze-drying after the AgI is filtered and separated; a pure product is obtained by recrystallizing the crude product in a system that the ratio of water to ethanol is 1:1. The anti-caner activity of the complex of the derivative is obviously higher than the oxaliplatin and the toxic side effect is obviously less than the oxaliplatin, and can be prepared into freeze-dried powders or injections and used for treating the cancer clinically.

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