单管法<sup>11</sup>C-CH<SUB>3</SUB>I的合成条件优化及胆碱生产与临床应用

单管法¹¹C-CH₃I的合成条件优化及胆碱生产与临床应用

摘要: 通过对合成¹¹C-CH₃I所用试剂的用量、反应的载气流量、压力和反应温度、蒸发时间等条件进行优化，进而用柱色层法合成了¹¹C-胆碱。在反应条件为：LiAlH₄和57% HI的用量分别为0.3 mL和0.5 mL，反应的最佳载气流量和压力分别为27 mL/min、0.28 kPa ，反应温度为180 ℃，蒸发时间为12 min下，¹¹C-CH₃I的校正后标记产率为62.2%±3.4%，放化纯度＞95%。临床脑胶质瘤和前列腺瘤疑似患者各1例在¹⁸F-FDG显像24 h后分别接受¹¹C-胆碱检查，并与¹⁸F-FDG显像结果对照。显像结果表明，¹⁸F-FDG检查示低代谢区¹¹C-胆碱均呈高代谢，联合用药可以更准确地区分病变的性质。

Abstract: The reaction conditions, including the amount of raw material, reaction temperature, evaporation time, pressure and flow rate of carrier gas for ¹¹C-CH₃I were investigated. The corrected yield of ¹¹CH₃I under optimized conditions (0.3 mL LiAlH₄, 0.5 mL 57% HI，0.28 kPa gas pressure, 27 mL/min carrier gas flow rate, 180 ℃ reaction temperature and 12 min evaporation time) was 62.2%±3.4% and the radiochemical purity was more than 95%. ¹¹C-choline PET/CT imaging in 2 patients was studied and compared with ¹⁸F-FDG PET/CT imaging. High uptake with ¹¹C-choline and low uptake with ¹⁸F-FDG in tumor were observed.