铂抗肿瘤药米铂的合成

Synthesis of Miriplatin,A Novel Platinum-Based Antitumor-Drug

目的合成铂类抗肿瘤新药米铂。方法以K4PtCl4为起始原料,将与亚硝酸钠反应生成的K4Pt(NO2)4溶液,与(1R,2R)-1,2-环己二胺反应生成顺式-二硝基-(1R,2R)-1,2-环己二胺合铂(II),使用硫酸肼还原NO2-根后将得到的溶液与正十四碳酸钠的正丁醇溶液反应生成米铂。采用元素分析、质谱、红外光谱、核磁共振氢谱、热分析和比旋光度对其结构进行表征。结果合成的化合物结构与标题化合物一致,产率约61%。结论本方法为米铂的合成提供了一条新型的工艺路线。

OBJECTIVE To synthesize the platinum-based anti-tumor drug miriplatin. METHODS Miriplatin was synthesized from K4PtC14. K4PtC14was reacted with sodium nitrite to give the K4Pt（ NO2 ）~ solution which reacted with（1R,2R）-1,2-cyclohexane- diamine thus resulting in the key intermediate Pt（ C6 H t~ N2 ） （NO2 ）2. The key intermediate was subsequently reacted with hydrazine sulfate and sodium myristate in n-butanol to give the target compound. The structure of the target compound was identified by elemental analysis, ESI-MS, FT-IR, 1H-NMR, thermal analysis and specific optical rotation measurement. RESULTS The structure of the synthesized compound was consistent with the title compound, and the yield was about 61%. CONCLUSION This study provides a novel synthesis process for miriplatin.