Synthesis of n.c.a. [188, 189, 191pt] Cisplatin From a Cyclotron-produced n.c.a. 188, 189, 191PtCl42- Complex

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<jats:title>Abstract</jats:title> <jats:p>We developed a novel method for production of no-carrier-added (n.c.a.) [<jats:sup>188, 189, 191</jats:sup>Pt]Pt<jats:sup>Ⅱ</jats:sup>Cl<jats:sub>4</jats:sub><jats:sup>2-</jats:sup> from an Ir target material, and then synthesized n.c.a. [*Pt]cis-[Pt<jats:sup>Ⅱ</jats:sup>Cl<jats:sub>2</jats:sub>(NH<jats:sub>3</jats:sub>)<jats:sub>2</jats:sub>] ([*Pt]cisplatin) from [*Pt]Pt<jats:sup>Ⅱ</jats:sup>Cl<jats:sub>4</jats:sub><jats:sup>2-</jats:sup>. [*Pt]Pt<jats:sup>Ⅱ</jats:sup>Cl<jats:sub>4</jats:sub><jats:sup>2-</jats:sup> 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<jats:sup>Ⅳ</jats:sup>Cl<jats:sub>6</jats:sub><jats:sup>2-</jats:sup> with ascorbic acid. The ligand-substitution reaction of Cl with NH<jats:sub>3</jats:sub> was promoted by treating n.c.a. [*Pt]Pt<jats:sup>Ⅱ</jats:sup>Cl<jats:sub>4</jats:sub><jats:sup>2-</jats:sup> with excess NH<jats:sub>3</jats:sub> 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).</jats:p>

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