Development of miniaturized synthesis modules for preparation of PET radiopharmaceuticals

开发用于制备 PET 放射性药物的小型化合成模块

• 批准号: 13470177
• 负责人: IWATA Ren
• 金额: $ 5.76万
• 依托单位: Tohoku University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (B)
• 财政年份: 2001
• 资助国家: 日本
• 起止时间: 2001 至 2003
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/en/grant/KAKENHI-PROJECT-13470177/
• 关键词: PET; Automated synthesis; Miniaturized synthesis module; Microreactor; Radiopharmaceutical; Labeling; マイクロリアクター; 比放射能

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.

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。

项目成果

R.Iwata, C.Pascali, A.Bogni, S.Furumoto, K.Terasaki, K.Yanai: "[^<18>F] Fluoromethyl triflate, a novel and reactive [^<18>F]fluoromethylating agent. Preparation and application to the on-column preparation of [^<18>F]fluorocholine"Applied Radiation Isotop

R.Iwata、C.Pascali、A.Bogni、S.Furumoto、K.Terasaki、K.Yanai：“[^18F]三氟甲磺酸甲酯，一种新型反应性[^18F]氟甲基化剂。制备

R. Iwata, C. Pascali, A. Bogni, K. Yanai, M. Kato, T. Ido, K. ishiwata: "A combined loop-SPE method for the automated preparation of [^<11>C]doxepin"J. Labelled Compounds and Radio pharmaceuticals. 45(印刷中). (2002)

R. Iwata、C. Pascali、A. Bogni、K. Yanai、M. Kato、T. Ido、K. ishiwata：“用于自动制备 [^11C] 多虑平的组合环 SPE 方法”J标记化合物和放射性药物 45（印刷中）。

R.Iwata, C.Pascali, A.Bogni, S.Furumoto, K.Terasaki, K.Yanai: "[^<18>F]Fluoromethyl triflate, a novel and reactive [^<18>F]fluoromethylating agent. Preparation and application to the on-column preparation of [^<18>F]fluorocholine"Applied Radiation Isotope

R.Iwata、C.Pascali、A.Bogni、S.Furumoto、K.Terasaki、K.Yanai：“[^18F]氟甲基三氟甲磺酸酯，一种新型反应性[^18F]氟甲基化剂。制备

Y.Funaki, M.Kato, R.Iwata, E.Sakurai, E.Sakurai, M.Tashiro, T.Ido, K.Yanai: "Evaluation of the binding characteristics of [5-^<11>C-methoxy]donepezil in the rat brain for in vivo visualization of acetylcholinesterase."J.Pharmacol.Sci.. 91. 105-112 (2003)

Y.Funaki、M.Kato、R.Iwata、E.Sakurai、E.Sakurai、M.Tashiro、T.Ido、K.Yanai：“[5-^<11>C-甲氧基]的结合特性评估

R.Iwata, C.Pascali, A.Bogni, Y.Miyake, K.Yanai, T.Ido: "A Simple Loop Method for the Automated Preparation of [^<11>C]Raclopride from [^<11>C]Methyl Triflate"Applied Radiation Isotopes. 55. 17-22 (2001)

R.Iwata、C.Pascali、A.Bogni、Y.Miyake、K.Yanai、T.Ido：“从 [^<11>C] 自动制备 [^<11>C]雷氯必利的简单循环方法