Journal of Isotopes ›› 2018, Vol. 31 ›› Issue (5): 304-309.DOI: 10.7538/tws.2018.31.05.

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Optimization of the Radiosynthesis of the Dopamine Transporter Imaging Agent of 11C-β-CFT

LI Haifeng1;XU Rengen1;LI Yungang2;CHEN Zhijun1;ZHANG Xiaojun2;ZHANG Jinming2   

  1. 1.Depatment of Nuclear Medicine, Jiang Xi Cancer Hospital, Nanchang 330029, China;2.Depatment of Nuclear Medicine, Chinese PLA General Hospital, Beijing 100853, China
  • Online:2018-10-20 Published:2020-08-14



  1. 1.江西省肿瘤医院 核医学科,南昌330029;2.中国人民解放军总医院 核医学科,北京100853


The optimization for high synthesis yield was designed with 11C-Triflate-CH3I as methylation agent for dopamine transporter imaging agent of 11C-β-CFT. The influence factors of the synthesis process were discussed, and the optimum synthetic conditions were established. In the paper, the study showed that the amount of precursor, the irradiation time, eluated condition, the reaction solvent etc could effect the synthetic efficiency. 11C-β-CFT was automatic synthesized on PET-CM-3H-IT-Ⅰ with the optimum process conditions as the irradiation time 10-24 minutes, 0.5-1.0 g/L of precursor in 0.2 mL acetone: acetonitrile(1∶1, VV) and room temperature. We obtained a radiochemical yield of (76.93±6.49)% (n=76, 11C-Triflate-CH3 EOB). The radiochemical purity of final products were over 97%. The specific activities of final products were over (56.26±1.55) TBq/g. It took 16 minutes from 11C-CO2 to 11C-β-CFT and the radio activity of 11C-β-CFT were (8.07±1.94) GBq (n=76). By optimization of the technological conditions, the target product was suitable for clinical, the synthetic process was reliable and full automated, the product yield was improved and the residual problem of Sep-Pak C18 was resloved.

Key words: 11C-β-CFT, full automated synthesis, PET/CT, quality control


本文以11C-Triflate-CH3为甲基化试剂合成多巴胺转运蛋白显像剂11C-β-CFT,探讨11C-β-CFT合成效率的影响因素,优化合成条件,提高其合成效率。使用国产合成模块PET-CM-3H-IT-Ⅰ全自动化合成11C-β-CFT,通过研究合成过程中反应溶剂、轰靶时间、前体量及淋洗终产品条件等影响因素,得到优化后11C-β-CFT的生产条件:轰靶时长10~24 min,前体浓度为0.5~1.0 g/L,以0.2 mL体积比V(丙酮)∶V(乙腈)=1∶1为溶剂,反应条件为室温。从传输11C-CO2到终产品的总合成时间为16 min,产量为(8.07±1.94) GBq(n=76);此条件下11C-β-CFT的合成效率为(76.93±6.49)%(n=76,11C-Triflate-CH3校正效率),产品的放化纯度大于97%,比活度(56.26±1.55) TBq/g。优化后的生产条件可以提高11C-β-CFT合成效率,解决了Sep-Pak C18柱残留产品过多的问题,可实现稳定、全自动化合成11C-β-CFT且保证产品满足临床需求。

关键词: 11C-β-CFT, 全自动化合成, PET/CT, 质量控制