制备奥沙利铂的一种新工艺

A New Technique for Synthesis of Oxaliplatin

目的改进抗肿瘤临床药物奥沙利铂的合成方法。方法用草酸亚汞和硝酸亚汞代替银盐来除去中间体[R(-NH2)2PtX2]中的配位卤离子。结果所得的Pt(Ⅱ)配合物经IR,1H-MMR,13C-NMR,EA和ESI-MS分析确证。结论该合成工艺纯度高,成本较低。

OBJECTIVE To study the synthetic process for oxaliplatin, an anti-tumor drug. METHODS Oxaliplatin was prepared by a new method. Mercurous ions in Hg2 （COO）2 or Hg2 （NO3）2instead of silver ones were used to remove the coordinating halide anions from the intermediate, [ R（ -NH2 ）2PtX2 ] . RESULTS The resulting platinum（Ⅱ） complex was identified by its infrared, ^1H-NMR,^13C-NMR and electrospray mass spectra together with elemental analyses. CONCLUSION This process is rather practical for the advantages of the high purity of products in fairly good yields and in low cost.