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从回旋加速器生产的 PtCl 复合物中合成无载体添加的[Pt]顺铂。

Synthesis of no-carrier-added [Pt]cisplatin from a cyclotron produced PtCl complex.

机构信息

Department of Advanced Nuclear Medicine Sciences, Institute for Quantum Medical Science (iQMS), National Institutes for Quantum and Radiological Science and Technology (QST), 4-9-1 Anagawa, Inage-ku, Chiba, 263-8555, Japan.

Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita-ku, Sapporo, Hokkaido, 060-0812, Japan.

出版信息

Sci Rep. 2021 Apr 14;11(1):8140. doi: 10.1038/s41598-021-87576-2.

Abstract

We developed a novel method for production of no-carrier-added (n.c.a.) [Pt]PtCl from an Ir target material, and then synthesized n.c.a. [*Pt]cis-[PtCl(NH)] ([*Pt]cisplatin) from [*Pt]PtCl. [*Pt]PtCl 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 IrCl with ascorbic acid. The ligand-substitution reaction of Cl with NH was promoted by treating n.c.a. [*Pt]PtCl with excess NH 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).

摘要

我们开发了一种从 Ir 靶材生产无载体添加(n.c.a.)[Pt]PtCl 的新方法,然后从 [*Pt]PtCl 合成了 n.c.a. [*Pt]顺式-[PtCl(NH)]([*Pt]顺铂)。[*Pt]PtCl 是通过用抗坏血酸选择性还原 IrCl 后,结合树脂萃取和阴离子交换色谱法制备的 n.c.a. *Pt 配合物的合成前体。通过用过量 NH 处理 n.c.a. [*Pt]PtCl 并加热反应混合物,促进了 Cl 与 NH 的配体取代反应,并且无需采用沉淀路线成功地生产了 n.c.a. [*Pt]顺铂。经过这种处理后,通过制备 HPLC 以放射性纯度 99+%在合成结束时(EOS)分离出 [*Pt]顺铂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d70f/8046966/369b0bcda7b8/41598_2021_87576_Fig1_HTML.jpg

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