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OPTICALLY HIGH-PURITY CIS-OXALATE (TRANS-L-1,2-CYCLOHEXANEDIAMINE) PLATINUM (II) COMPLEX AND ITS PRODUCTION

机译:光学级高纯度顺式草酸(TRANS-L-1,2-环己二胺)铂(II)配合物及其生产

摘要

PURPOSE:To obtain a optically high-purity cis-oxalate(trans-1,1,2- cyclohexanediamine)platinum (II) complex useful as an original medicine for carcinostatic agent, etc., showing anticancer properties, having no toxicity, prepared from trans-1-1,2-cyclohexanediamine optically resolved by high- performance liquid chromatography. CONSTITUTION:trans-1-1,2-Cyclohexanediamine optically resolved by high- performance liquid chromatography or its derivative is used as a raw material and reacted with a tetravalent platinate (e.g. potassium chloroplatinate) to give a tetrahalogeno(trans-1-1,2-cyclohexanediamine)platinum (IV) complex of formula I (X is halogen). Then, the platinum complex is suspended in water, reacted with silver oxalate to give the objective cis-oxalate(trans-1-1,2- cyclohexanediamine)platinum (II) complex of formula II, showing anti-cancer properties but not toxicity, =99.94%e.e. optical purity and 198.3-199.7 deg.C melting point.
机译:目的:获得一种光学上高纯度的顺式草酸(反式1,1,2-环己二胺)铂(II)络合物,该化合物可用作抗癌剂等的原始药物,其显示抗癌特性,无毒,由通过高效液相色谱光学拆分反式-1-1,2-环己二胺。组成:以高效液相色谱法光学拆分的反式-1-1,2-环己二胺为原料,与四价铂酸盐(例如氯铂酸钾)反应,生成四卤代(反式1-1,式I的2-环己二胺)铂(IV)配合物(X是卤素)。然后,将铂配合物悬浮在水中,与草酸银反应,生成目标式II的顺式草酸(反式1-2-环己二胺)铂(Ⅱ)配合物,显示出抗癌特性,但没有毒性, > = 99.94%ee光学纯度和198.3-199.7℃熔点。

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