Optimization for the Synthesis Efficiency of the 11C-Raclopride

doi:10.7538/tws.2016.29.01.0012

Abstract

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-CO₂to 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

LI Hai-feng;CHEN Zhi-jun;ZHANG Xiao-jun;LI Yun-gang;ZHANG Jin-ming. Optimization for the Synthesis Efficiency of the ¹¹C-Raclopride[J]. JOURNAL OF ISOTOPES, DOI: 10.7538/tws.2016.29.01.0012.

李海峰;陈志军;张晓军;李云钢;张锦明. ¹¹C标记雷氯必利合成效率的影响因素[J]. 同位素, DOI: 10.7538/tws.2016.29.01.0012.

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Optimization for the Synthesis Efficiency of the ¹¹C-Raclopride

¹¹C标记雷氯必利合成效率的影响因素

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