(N-[^(11)C]甲基)胆碱和(S-[^(11)C]甲基)-L-半胱氨酸的半自动合成  

Semi-automated synthesis of (N-[^(11)C]methyl)choline and (S-[^(11)C]methyl)-L-cysteine

作　　者：唐刚华[1] 王明芳[1] 唐小兰[2] 罗磊[1] 甘满权[1] 

机构地区：[1]南方医科大学南方医院南方PET中心,广州510515 [2]华南农业大学理学院,广州510642

出　　处：《核技术》2005年第6期454-457,共4页Nuclear Techniques

基　　金：广东省科技计划项目(2003C34304);南方医科大学南方医院院长基金资助项目(991015)资助

摘　　要：由PETtrace回旋加速器和11CH3I全自动合成系统分别生产11CO2和11CH3I;;采用半自动合成装置合成(N-[11C]甲基)胆碱(11C-CH)和(S-[11C]甲基)-L-半胱氨酸(11C-CYS)。11CH3I与前体N;;N-二甲基乙醇胺在Sep-PakPlusC18小柱中发生甲基化反应;;经AccellSep-PakPlusCM小柱分离;;得11C-CH注射液;;11CO2转化为11C-CH总时间约20min;;校正总放化产率大于85%;;放化纯度大于99%。11CH3I与前体L-半胱氨酸在Sep-PakPlusC18小柱中发生甲基化反应;;经SepPakPlusC18小柱分离;;得11C-CYS注射液;;烷基化时间约6min;;放化产率大于85%;;放化纯度大于99%;;对映纯度大于90%。制备的11C-CH和11C-CYS注射液可用于动物和人体研究。11CH3I was produced at 11CH3I MicroLab Fully Automated Process Module from 11CO2, which was produced via nuclear reaction 14N(p, α)11C at PETtrace Cyclotron. (N-[11C]methyl)choline (11C-CH) was synthesized from [11C]methylation of precursor (CH3)2 NCH2CH2OH with 11CH3I on a commercial Sep-Pak Plus C18 cartridge as a solid-phase support material at a semi-automated system and separated by Accell Sep-Pak Plus CM. The corrected radiochemical yield of 11C-CH from 11CO2 was more than 85% with the total synthesis time about 20 min and the radiochemical purity above 99%. (S-[11C]Methyl)-L-cysteine (11C-CYS) was synthesized from [11C]methylation of precursor L-cysteine with 11CH3I on a Sep-Pak Plus C18 cartridge at the semi-automated system. The uncorrected radiochemical yield of 11C-CYS from 11CH3I was more than 85% with the synthesis time about 6 min, the radiochemical purity of 11C-CYS was above 99%, and the enantiomeric purity was over 90%. The synthetic 11C-CH and 11C-CYS injection can be used for preclinical and clinical study with PET imaging.

关 键 词：^11CH3I全自动合成系统 (N-[^11C]甲基)胆碱 (S-[^12C]甲基)-L-半胱氨酸 在柱甲基化 半自动合成 

分 类 号：R916.41[医药卫生—药学] O615.9[理学—无机化学]