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为合成抗肿瘤药物甲啶铂,采用醋酸铵与K2PtCl4反应生成K[Pt(NH3)Cl3],再先后与碘化钾、2-甲基吡啶、硝酸银、氯化钾反应生成甲啶铂。采用元素分析、质谱、核磁共振氢谱和红外光谱对其结构进行了表征。结果显示合成的化合物与理论一致,产率约为40%,可为甲啶铂的合成提供一条新的工艺路线。

To synthesize a platinum-based anti-tumor drug picoplatin, the key intermediate K[Pt(NH3)Cl3] , synthesized from ammonium acetate and K2PtCl4 was subsequently reacted with KI, 2-picoline, AgNO3 and KCl to give the target compound. The structure and component were characterized by elemental analysis, ESI-MS, 1H-NMR and IR. The results showed that its structure was consistent with the title compound and the yield was about 40%. This provides a new process for the synthesis of picoplatin.

参考文献

[1] Dou Illard J Y;Schiller J .ZD0473 combined with other chemotherapeutic agent for the treatment of solid malignancies[J].Eur J Camcer,2002,38(S):25-31.
[2] Anneli O;Markku L .Synthesis of ammonium trichloro-monoammineplatinate(II)improved through control of temperature[J].Acta Chemica Scandinavica,1994,48:485-489.
[3] Rochon F D;Kong P C .Iodo-bridged complexes of platinum(II)and synthesis of cis mixed-amine platinum(II)compounds[J].Canadian Journal of Chemistry,1986,64:1894-1896.
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