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Remote-controlled module-assisted synthesis of O-(2-[18^F]fluoroethyl)-L-tyrosine as tumor PET tracer using two different radiochemical routes
作者姓名:WANG  Ming-Wei  YIN  Duan-Zhi  ZHANG  Lan  ZHOU  Wei  WANG  Yong-Xian
作者单位:Radiopharmaceutical Centre, Shanghai Institute of Applied Physics, the Chinese Academy of Sciences, Shanghai 201800, China
基金项目:中国科学院知识创新工程项目 , 国家自然科学基金
摘    要:The positron-emitter fluorine-18 labeled amino acid O-(2-18^F]fluoroethyl)-L-tyrosine (18^F]FET) has shown very promising perspectives for brain tumor diagnosis with positron emission tomography (PET). There have been two existing preparation routes of 18^F]FET named direct nucleophilic radiofluofination of protected L-tyrosine and radiofluoroalkylation of unprotected L-tyrosine, respectively. A general module was designed specifically for the routine synthesis of 18^F]FET, which could be suitable for the present two chemical methods with simple modifications. The fluorinated intermediates and the final product were separated and purified using solid phase extraction (SPE) on the Sep-Pak silica plus cartridge instead of the time-consuming high performance liquid chromatography (HPLC) procedures. The total synthesis time was about 50-60 min with good radiochemical yield (about 20-40%, no-decay-corrected) and good radiochemical purity (more than 97%) for both the synthetic methods.

关 键 词:PET  氟化作用  合成模块  正电子发射  亲质子
收稿时间:2006-02-22

Remote-controlled module-assisted synthesis of O-(2-[F]fluoroethyl)-L-tyrosine as tumor PET tracer using two different radiochemical routes
WANG Ming-Wei YIN Duan-Zhi ZHANG Lan ZHOU Wei WANG Yong-Xian.Remote-controlled module-assisted synthesis of O-(2-[F]fluoroethyl)-L-tyrosine as tumor PET tracer using two different radiochemical routes[J].Nuclear Science and Techniques,2006,17(3):148-153.
Authors:WANG Ming-Wei  YIN Duan-Zhi  ZHANG Lan  ZHOU Wei  WANG Yong-Xian
Affiliation:Radiopharmaceutical Centre, Shanghai Institute of Applied Physics, the Chinese Academy of Sciences, Shanghai 201800, China
Abstract:The positron-emitter fluorine-18 labeled amino acid O-(2-18F]fluoroethyl)-L-tyrosine (18F]FET) has shown very promising perspectives for brain tumor diagnosis with positron emission tomography (PET). There have been two existing preparation routes of 18F]FET named direct nucleophilic radiofluorination of protected L-tyrosine and radiofluoroalkylation of unprotected L-tyrosine, respectively. A general module was designed specifically for the routine synthesis of 18F]FET, which could be suitable for the present two chemical methods with simple modifications. The fluorinated intermediates and the final product were separated and purified using solid phase extraction (SPE) on the Sep-Pak silica plus cartridge instead of the time-consuming high performance liquid chromatography (HPLC) procedures. The total synthesis time was about 50-60min with good radiochemical yield (about 20 40%,no-decay-corrected) and good radiochemical purity (more than 97%) for both the synthetic methods.
Keywords:[18F]FET  PET  Fluorination  Fluoroalkylation  Synthesis module
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