抗肿瘤药奥沙利铂的合成工艺改进

Improved synthesis of antitumor drug oxaliplatin

目的合成抗肿瘤药物奥沙利铂。方法以氯亚铂酸钾为起始原料,先后与亚硝酸钠、(1R,2R)-环己二胺、硫酸肼、一水合草酸钾反应合成目标化合物。合成的化合物采用元素分析、质谱、红外光谱、核磁共振氢谱和比旋光度对其结构进行表征。结果与结论合成的化合物结构与标题化合物一致,精品收率为52%。本方法为奥沙利铂的合成提供了一条新型的工艺路线。

The preparation of platinum-based antitumor drug oxaliplatin was achieved via a four-step sequence from K4PtCl4. K4PtCl4 was treated with sodiunmitrite to give the K4Pt（ NO2 ）4 solution, then which was reacted with（ 1R ,2R） -1,2-cyclohexanediamine to give the key intermediate Pt（ C6H14N2 ） （ NO2 ） 2. The key intermediate was subsequently reacted with hydrazine sulfate and potassium oxalate monohydrate to give target compound. The structure of the target compound was identified by elemental analysis, ESI-MS, FT-IR, 1H-NMR and specific rotatory power. The result showed that its structure was consistent with the title compound,the yield was about 52%. This article provides a novel process for the praparation of oxaliplatin.