Development of miniaturized synthesis modules for preparation of PET radiopharmaceuticals

首先简化了PET放射性药物的制备过程，实现了自动化高效合成，然后利用多个微型阀开发了小型化合成模块。1.成功地将Loop方法和固相萃取相结合，实现了受体配体的高效在线[^<11>C]甲基化处理和HPLC纯化。以[^<18>F]氟化物为原料，合成了一种新型的[^F]标记剂[^ F]氟甲基三氟<18><18>甲磺酸酯，并成功应用于[^<18>F]氟胆碱和[^<18>F]氟甲基酪氨酸的合成。利用该技术开发了适合于常规制备[^<11>F]蛋氨酸和[^<11>F]胆碱的微型化模块。4.还开发了用于从<18>[^ F]氟化物制备[^ F]氟甲基三氟<18>甲磺酸酯和[^<18>F]氟胆碱的柱上制备的微型化合成模块。

Procedures for the preparation of useful PET radiopharmaceuticals were first simplified for automated efficient synthesis and then miniaturized synthesis modules were developed using manifold miniature valves.1.Loop method and solid phase extraction were successfully combined for efficient on-line processing of [^<11>C]methylation and HPLC purification of receptor ligands.2.[^<18>F]Fluoromethyl triflate, a novel ^<18>F-labeling agent, was prepared from [^<18>F]fluoride and successfully applied to the synthesis of [^<18>F]fluorocholine and [^<18>F]fluoromethyl tyrosine.3.A new synthesis module of a palm size was developed for the first time using miniature manifold valves. Using this technique a miniaturized module suitable for routine preparation of [^<11>C]methionine and [^<11>C]choline was developed.4.Synthesis modules were also miniaturized for the preparation of [^<18>F]fluoromethyl triflate from [^<18>F]fluoride and the on-column preparation of [^<18>F]fluorocholine.