On-line [11C]methylation using [11C]methyl iodide for the automated preparation of 11C-radiopharmaceuticals

International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes Pub Date : 1992-09-01 DOI:10.1016/0883-2889(92)90048-J

Ren Iwata , Claudio Pascali , Mitsuaki Yuasa , Kazuhiko Yanai , Toshihiro Takahashi , Tatsuo Ido

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引用次数: 30

Abstract

A novel method for the efficient preparation of ¹¹C-radiopharmaceuticals by on-line [¹¹C]methylation using [¹¹C]methyl iodide has been developed and applied to a rapid, convenient automated system. [¹¹C]Methyl iodide is first trapped in a short column, containing an adsorber and coated substrate, which is connected to an HPLC injector. DMF is then introduced. Alternatively the substrate is added with the DMF. A whole reaction mixture can be easily injected onto an HPLC column for purification by switching the injector valve immediately after the reaction. Thus, radiochemical yields in the preparation of ¹¹C-labeled doxepin, benztropine, cyproheptadine and N-methylspiperone have been improved remarkably and the synthetic procedure simplified.

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使用[11C]甲基碘化物进行在线[11C]甲基化，用于自动制备11C-放射性药物

本文提出了一种利用碘化甲基在线甲基化制备11C-放射性药物的新方法，并将其应用于快速、方便的自动化系统中。[11C]碘化甲酯首先被捕获在一个短柱中，该短柱包含一个吸附器和被涂覆的底物，该底物与HPLC进样器相连。然后介绍DMF。或者，将底物与DMF一起添加。整个反应混合物可以很容易地注入到高效液相色谱柱上进行纯化，只需在反应后立即切换进样阀即可。从而显著提高了11c标记的多塞平、苯托品、赛庚啶和n -甲基哌替酮的放射化学收率，简化了合成过程。

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International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes

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