在柱甲基化法自动合成(S-[^(11)C]甲基)-L-蛋氨酸和(S-[^(11)C]甲基)-L-半胱氨酸  

Automated Synthesis of (S-[^(11)C]-methyl)-L-methionine and (S-[^(11)C]-methyl)-L-cysteine by On-column [^(11)C]methylation

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]第一军医大学南方医院南方PET中心,广东广州510515 [2]华南农业大学理学院,广东广州510642

出　　处：《核化学与放射化学》2004年第2期77-83,共7页Journal of Nuclear and Radiochemistry

基　　金：广东省科技计划资助项目(2003C34304);第一军医大学南方医院院长基金资助项目(991015)

摘　　要：用PETtrace回旋加速器通过核反应14N(p,α)11C生产11CO2,经甲烷循环碘化法和11CH3I全自动合成系统制备11CH3I,合成时间约为12min,未校正放化产率大于30%。采用(S [11C]甲基) L 蛋氨酸(11C MET)半自动合成装置,使11CH3I与前体L 同型半胱氨酸硫内酯盐酸盐的碱性溶液在SepPakPlusC18小柱上发生烷基化反应,并经SepPakPlusC18小柱分离,得11C MET注射液,烷基化反应时间约6min,放化产率大于85%,放化纯度大于99%,对映纯度约为90%。采用PET CS I型全自动合成模块,使11CH3I与前体L 半胱氨酸发生在柱烷基化反应,并经柱分离后得到(S [11C]甲基) L 半胱氨酸(11C CYS)注射液,烷基化反应时间约2min,未校正放化产率大于50%,放化纯度大于99%,对映纯度大于90%。制得的11C MET和11C CYS注射液可用于动物和人体研究。After^(11)CO_2 is produced via nuclear reaction^(14)N(p,α)^(11)C at a PET trace cyclotron,^(11)CH_3I is synthesized from the hydrogenation of^(11)CO_2 by catalyst Ni and the recycle iodination of^(11)C-CH_4 at^(11)CH_3I Micro Lab Process Module, with uncorrected radiochemical yield more than 30% in the synthesis time about 12 min. (S-[^(11)C]-methyl)-L-methionine (^(11)C-MET) is synthesized from [^(11)C]methylation of^(11)CH_3I with precursor L-homocysteine thiolactone hydrochloride in NaOH solution on a commercial C18 Sep-Pak Plus cartridge as a solid-phase support material at the semi-automated system for the synthesis of^(11)C-MET. The corrected radiochemical yield of [(^(11)C)]methylation is more than 85% with the synthesis time about 6 min, the radiochemical purity of^(11)C-MET is above 99%, and the enantiomeric purity is about 90%. (S-[(^(11)C)]-methyl)-L-cysteine ((^(11)C)-CYS) is synthesized from [(^(11)C)] methylation of(^(11)CH_3I) with precursor L-cysteine on a commercial cartridge as a solid-phase support material at the PET-CS-I model fully automated system. The uncorrected radiochemical yield of^(11)C-CYS from^(11)CH_3I is more than 50% with the synthesis time about 2 min, the radiochemical purity of^(11)C-CYS is above 99%, and the enantiomeric purity is over 90%. The synthetic^(11)C-MET and^(11)C-CYS injections can be suitable for preclinical and clinical study with PET imaging.

关 键 词：在柱甲基化法 自动合成 (S-[^11C]甲基)-L-蛋氨酸 (S-[^11C]甲基)-L-半胱氨酸 肿瘤氨基酸代谢正电子发射断层显像 显像剂 全自动合成 

分 类 号：R730[医药卫生—肿瘤]