New Method for Synthesis of ¹⁸F-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).