Synthesis of no-carrier-added [(188, 189, 191)Pt]cisplatin from a cyclotron produced (188, 189, 191)PtCl(4)(2-) complex

利用回旋加速器产生的(188, 189, 191)PtCl(4)(2-)配合物,合成无载体添加的[(188, 189, 191)Pt]顺铂。

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Abstract

We developed a novel method for production of no-carrier-added (n.c.a.) [(188, 189, 191)Pt]Pt(II)Cl(4)(2-) from an Ir target material, and then synthesized n.c.a. [*Pt]cis-[Pt(II)Cl(2)(NH(3))(2)] ([*Pt]cisplatin) from [*Pt]Pt(II)Cl(4)(2-). [*Pt]Pt(II)Cl(4)(2-) was prepared as a synthetic precursor of n.c.a. *Pt complex by a combination of resin extraction and anion-exchange chromatography after the selective reduction of Ir(IV)Cl(6)(2-) with ascorbic acid. The ligand-substitution reaction of Cl with NH(3) was promoted by treating n.c.a. [*Pt]Pt(II)Cl(4)(2-) with excess NH(3) and heating the reaction mixture, and n.c.a. [*Pt]cisplatin was successfully produced without employing precipitation routes. After this treatment, [*Pt]cisplatin was isolated through preparative HPLC with a radiochemical purity of 99 + % at the end of synthesis (EOS).

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