Remote-controlled module-assisted synthesis of O-(2-[^(18)F]fluoroethyl)-L-tyrosine as tumor PET tracer using two different radiochemical routes  

作　　者：WANG Ming-Wei YIN Duan-Zhi ZHANG Lan ZHOU Wei WANG Yong-Xian 

机构地区：[1]Radiopharmaceutical Centre, Shanghai Institute of Applied Physics, the Chinese Academy of Sciences, Shanghai 201800, China

出　　处：《Nuclear Science and Techniques》2006年第3期148-153,共6页核技术（英文）

基　　金：SupportedbytheKnowledgeInnovationProjectofChineseAcademyofSciences(No.KJCX1-SW-08)andtheNationalNaturalScienceFoundationofChina(No.30371634).

摘　　要：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 modifica- tions. 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.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 

分 类 号：O621.3[理学—有机化学]