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(N-[11C]甲基)胆碱和(S-[11C]甲基)-L-半胱氨酸的半自动合成
Semi-automated synthesis of (N-[11C]methyl)choline and (S-[11C]methyl)-L-cysteine
【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。
【Abstract】 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)2NCH2CH2OH 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.
【Key words】 11CH3I MicroLab Process Module; (N-[11C]Methyl)choline; (S-[11C]Methyl)-L-cysteine; On-column methylation; Semi-automated synthesis;
- 【文献出处】 核技术 ,Nuclear Techniques , 编辑部邮箱 ,2005年06期
- 【分类号】R914
- 【被引频次】2
- 【下载频次】91