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.

首先简化了有用的 PET 放射性药物的制备程序，以实现自动化高效合成，然后使用多种微型阀门开发了小型化合成模块。1.成功地将循环方法和固相萃取相结合，实现了 [^<11>受体配体的C]甲基化和HPLC纯化。2.[^ 18 F]氟甲基三氟甲磺酸酯，一种新型^ 18 F-标记剂，由[^<18>F]氟化物并成功应用于[^<18>F]氟胆碱和[^<18>F]氟甲基酪氨酸的合成。3.首次开发了手掌大小的新型合成模块使用微型歧管阀。使用该技术，开发了适合常规制备[^ 11 C]甲硫氨酸和[^ 11 C]胆碱的小型化模块。4.合成模块也被小型化，用于制备[^ 18 F]氟甲基来自[^ 18 F]氟化物的三氟甲磺酸酯和[^ 18 F]氟胆碱的柱上制备。

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