Iwata R, Pascali C, Yuasa M, Yanai K, Takahashi T, Ido T
CYRIC Tohoku University, Sendai, Japan.
Int J Rad Appl Instrum A. 1992 Sep;43(9):1083-8. doi: 10.1016/0883-2889(92)90048-j.
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.
已开发出一种通过使用[¹¹C]碘甲烷进行在线[¹¹C]甲基化来高效制备¹¹C放射性药物的新方法，并将其应用于快速、便捷的自动化系统。首先将[¹¹C]碘甲烷捕集在一个短柱中，该短柱包含吸附剂和涂覆的底物，且与HPLC进样器相连。然后引入DMF。或者将底物与DMF一起加入。反应结束后立即切换进样器阀，整个反应混合物即可轻松注入HPLC柱进行纯化。因此，¹¹C标记的多塞平、苯海索、赛庚啶和N-甲基螺哌隆的制备中的放射化学产率得到了显著提高，合成步骤也得以简化。
