奈达铂的新合成方法、晶体结构和热稳定性

Synthesis,Crystal Structure and Thermal Stability of A Platinum-Based Anti-Tumour Drug Nedaplatin

本文报道了铂族金属抗癌药物奈达铂的一种新合成方法,产率约65%,精品含量超过99%。采用了元素分析、红外光谱、质谱、差热-热重分析和X射线衍射手段对其结构和组成进行了表征。该配合物的晶体属正交晶系,空间群P212121。单晶X射线衍射结构分析结果表明铂髤离子与2个氨分子的氮原子以及乙醇酸羟基和羧基的氧原子配位,形成平面正方形结构,乙醇酸的二价阴离子通过羟基和羧基上的氧原子与铂髤离子配位形成五原子的螯合物。经TG-DTA分析显示奈达铂在低于180℃时稳定。

The nedaplatin has been synthesized by a new technique, the yield rate is about 65%, the content of pure product is above 99%. Its structure was characterized by elemental analysis, IR, MS, thermal analysis and X-ray diffraction single crystal structure analysis. Its crystal belongs to orthorhombic space group P212121 with a= 0.562 93（6） nm, b=0.728 53（8） nm, c=1.411 07（16） nm. The Pt^Ⅱ atom is coordinated by two N atoms of ammine and two O atom of carboxyl group and hydroxy, forming a sqare-planar environment. The glycolate dianion forms a fivemembered chelate ring, coordinating to the Pt（lI） ion not only at an O atom of the carboxyl group but also at the hydroxy. The results of TG-DTA analysis show that the nedaplatin was stable under 180℃. CCDC： 706387.