Development of miniaturized synthesis modules for preparation of PET radiopharmaceuticals

制备有用的PET放射性药物的程序首先简化为自动化高效合成，然后使用多种微型阀开发了小型化合成模块。环法和固相萃取法成功结合，实现了[^<11>C]甲基化的在线处理和受体配体的高效液相色谱纯化。以[^<18>F]氟为原料制备了一种新型的^<18>F标记剂氟甲基三氟酸酯，并成功地应用于[^<18>F]氟胆碱和[^<18>F]氟甲基酪氨酸的合成。一个新的合成模块的手掌大小的首次开发使用微型歧管阀。利用该技术研制了适合常规制备[^<11>C]蛋氨酸和[^<11>C]胆碱的小型化模块。合成模块也被小型化，用于从[^<18>F]氟中制备[^<18>F]氟甲基三氟酸盐和在柱上制备[^<18>F]氟胆碱。

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.