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Optimization for the Synthesis Efficiency of the 11C-Raclopride

LI Hai-feng1;CHEN Zhi-jun1;ZHANG Xiao-jun2;LI Yun-gang2;ZHANG Jin-ming2   

  1. 1.Department of Nuclear Medicine, Jiang Xi Cancer Hospital, nanchang 330029, China;2.Department of Nuclear Medicine, The PLA General Hospital, Beijing 100853, China
  • Online:2016-02-20 Published:2016-03-01

11C标记雷氯必利合成效率的影响因素

李海峰1;陈志军1;张晓军2;李云钢2;张锦明2   

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

Abstract:

The synthesis conditions of the 11C-Raclopride with domestic PET-CM-3H-IT-I synthesis module and 11C-Triflate-CH-3I as methylation agent were studied, which included the alkali equivalent, solvents, temperature, the amount of precursor and elution conditions for the product. The optimum condition was 1.5-3.0 g/L of precursor in acetone (0.2 mL), alkali equivalent (0.30-1.25 eq) and at room temperature (25 ℃) for synthesis of 11C-Raclopride. It could be got with radiochemical yield of (64.82±4.74)% (n=46, EOB of 11C-Triflate-CH3). The radiochemical purity was over 97% and the specific activity was at (423.61±13.43) GBq/g. It took 23 minutes from 11C-CO2 to 11C-Raclopride, and the production radioactivity was (6.9±0.87) GBq (n=46). The synthetic process was reliable and reproducible, and the product synthesized by this process was suitable for clinical use.

Key words: 11C-Raclopride, synthesis efficiency, PET/CT

摘要:

本文以11C-Triflate-CH3为甲基化试剂,使用国产模块 PET-CM-3H-IT-I合成11C标记化合物雷氯必利(11C-Raclopride),研究其合成过程中的碱量、溶剂、反应温度、前体量及产品淋洗条件对合成效率的影响,优化11C-Raclopride的合成条件。优化后的合成条件为:以0.2 mL丙酮为溶剂,前体浓度1.5~3.0 g/L,反应温度为室温(25 ℃),碱量0.30~1.25 eq,11C-Raclopride的合成效率(64.82±4.74)% (n=46,以11C-Triflate-CH3计校正效率),产品的放化纯度大于97%,比活度为(423.61±13.43) GBq/g,从收集11C-CO2至得到11C-Raclopride终产品的总合成时间为23 min,产量(6.9±0.87) GBq(n=46)。通过优化合成工艺,实现了稳定性和重复性良好的全自动化合成11C-Raclopride,且产品满足临床使用需要。

关键词: 11C-雷氯必利, 合成效率, PET/CT