抗肿瘤药米铂的一种新合成方法及结构表征

目的 合成抗肿瘤新药米铂。方法 以顺式- (1R，2R)-1, 2-环己二胺-二碘合铂(II)为起始原料，先将顺式- (1R，2R)-1, 2-环己二胺-二碘合铂(II)与硫酸银水解成含有硫酸根的水合物溶液，然后与八水氢氧化钡反应生成顺式- (1R，2R)-1,2-环己二胺-二羟基合铂(II)的水溶液，最后与正十四碳酸的正丁醇溶液反应合成米铂。采用元素分析、质谱、红外光谱、核磁共振氢谱和热分析对其结构进行表征。结果与结论 合成的化合物结构与标题化合物一致，收率约68%。该方法便于操作，收率高，可做进一步研究。

A new synthetic method and characterization of miriplatin,an antitumor drug

Miriplatin(1), a novel lipophilic platinum complex has been developed to treat hepatocellular carcinoma. A new synthetic route was designed and used to prepare the target compound. The key intermediate Pt(C₆H₁₄N₂)(OH)₂(2) ,synthesized from Pt(C₆H₁₄N₂)I₂ with AgNO₃ and Ba(OH)_2·8H₂O, was subsequently reacted with CH₃(CH₂)₁₂COOH in n-butanol to give target compound with satisfied yield 68%(based on Pt(C₆H₁₄N₂)I₂). The structure of the target compound was identified by elemental analysis, ESI-MS, FT-IR, ¹H-NMR and thermal analysis. And the structure was consistent with the target compound. Compared with reported methods, the new starting compound Pt(C₆H₁₄N₂)I₂ replacing the Pt(C₆H₁₄N₂)Cl₂ is convenient for controlling the Ag⁺, and using n-butanol-H₂O as the reaction medium can achieve a desirable reaction rate, however a large amount of CH₃(CH₂)₁₂COONa in the product was not easy to be removed . In addition, using n-butanol is less harmful than chloroform to human body.