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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

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【作者】 唐刚华; 王明芳; 唐小兰; 罗磊; 甘满权;

【Author】 TANG Ganghua1 WANG Mingfang1 TANG Xiaolan2 LUO Lei1 GAN Manquan1 1(Nanfang PET Centre, Nan Fang Hospital, Southern Medical University, Guangzhou 510515, China) 2(College of Science, South China Agricultural University, Guangzhou 510642, China)

【机构】 南方医科大学南方医院南方PET中心; 华南农业大学理学院; 南方医科大学南方医院南方PET中心 广州510515; 广州510515; 广州510642; 广州510515;

【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.

【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
  • 【分类号】R914
  • 【被引频次】2
  • 【下载频次】91
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