~(18)F-乙基胆碱(~(18)F-FECH)合成新工艺

~(18)F-甲基胆碱(~(18)F-FCH)和~(18)F-乙基胆碱(~(18)F-FECH),是两种重要的~(18)F标记的胆碱类似物,它们既被磷酸激酶磷酸化,又参与膜磷脂的合成,广泛应用于正电子发射计算机断层显像(PET-CT)检查,在肿瘤诊断中具有十分重要的作用。但普遍存在合成产率不高、不稳定或者使用对皮肤具有腐蚀性的三氟甲磺酸银(triflate-Ag),为合成操作和临床应用带来不便。本工作以2-溴三氟甲磺酸乙酯(BrC_2H_4OTf)与~(18)F-反应生成BrC_2H_4~(18)F,再与N,N-二甲基乙醇胺反应,纯化后得到产品。改变了传统工艺中以价格比较昂贵的TsOCH_2CH_2TsO为原料的方法,避免腐蚀性较强的三氟甲磺酸银(triflate-Ag)柱的CH_2Br_2的方法。反应过程温和,各个反应步骤容易控制,对合成模块设备的要求较低,合成时间短,利于~(18)F-乙基胆碱(~(18)F-FECH)的临床应用。

New Method for Synthesis of18F-Fluoroethylcholine

¹⁸F-fluoromethylcholine and ¹⁸F-fluoroethylcholine are two important ¹⁸F-labeled choline analogues. They could be phosphorylated by phosphokinase, involving in the synthesis of membrane phospholipids, which are widely used in PET-CT, and also playing an important role in tumor diagnosis. However, the low yield, instability, and the use of corrosive trichomethanesulfonate(triflate-Ag) increased the difficulty of the synthesis, operation and clinical application. In this paper, BrC₂H₄¹⁸F was prepared by 2-bromo-trifluoromethanesulfonate (BrC₂H₄OTf) and ¹⁸F^-, and then it reacted with N, N-dimethylethanolamine ion. After purification, the product was obtained. The traditional process was changed to avoid the corrosive triflomethanesulfonate(triflate-Ag) column CH₂Br₂ method, while the expensive TsOCH₂CH₂TsO was not used as the raw material. The reaction process is mild and the reaction steps are easy to control. The low requirements of the synthesis module and short synthesis time are beneficial to the clinical application of ¹⁸F-choline (¹⁸F-FECH).