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.

首先简化了用于制备有用PET放射性药物的程序以进行自动合成，然后使用歧管微型阀开发了微型合成模块。1.1.Loop方法和固相提取成功地结合了[^<11> c]甲基化和Hplc Fulorifients的在线处理，以有效地在线处理。 Triflate是一种新型^<18> f标记的剂，由氟化氟化物制备，并成功地应用于[^^<18> f]氟胆碱的合成和[^^<18> f]荧光甲基酪氨酸。3.aPalm size的新合成模块的首次使用Miniature Carecorltes开发了Palm大小的新合成模块。使用此技术，开发了适合常规制备[^<11> c]蛋氨酸和[^<11> c]胆碱的微型模块。4。还将相同模块微型化，以制备[^<18> f]氟甲基三酯的氟化物中的氟化物和氟化物的氟甲基三脂，

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

S.Furumoto, R.Iwata, T.Ido: "Design and synthesis of fluorine-18 labeled matrix metalloproteinase inhibitors for cancer imaging"J.Labeled.Compounds and Radiopharmaceuticals. 45. 975-986 (2002)

S.Furumoto、R.Iwata、T.Ido：“用于癌症成像的氟 18 标记基质金属蛋白酶抑制剂的设计和合成”J.Labeled.Compounds and Radiopharmaceuticals。