- 期刊
【論文摘要】An Improved Purification of [F-18]FEONM for Tau Protein Imaging
摘要
Introduction: 2-(1-{6-[(2-2'-[F-18]fluoroethoxyethyl) (methyl)amino]-2-naphthyl}-ethylidene)malononitrile ([F-18]FEONM) is a new Tau protein imaging agent. Originally, it was synthesized by radiofluorination of its precursor with K[F-18]/K2.2.2 at 110°C followed by purification with solid phase extraction (SPE) [1]. However, the chemical purity of [F-18]FEONM purified by SPE is relative low (Figure 1). In order to improve the chemical purity and decrease the toxicity of [F-18]FEONM injection, we have developed and reported herein a high performance liquid chromatogaphy (HPLC) system to purify [F-18]FEONM. Methods: [F-18]FEONM was synthesized by radio-fluorination of its precursor with K[F-18]/K2.2.2 at 95°C for 15 min. The reaction mixture was cooled to room temperature and injected into HPLC (column: Fortis diphenyl HPLC column; length: 250 mm; diameter: 10 mm; eluent: 95% ethanol [EtOH]; flow rate: 1.6 ml/min). The peak corresponding to [F-18]FEONM was collected, diluted with saline to make EtOH concentration ＜ 10% and passed through Millipore filter into a multi-injection vial. Results: The non-decay-corrected radiochemical yield of [F-18]FEONM synthesized by this method is 15-20% in a synthesis time of 70 min from end of bombardment (EOB). The radiochemical and chemical purities are higher than 95% as detected by HPLC and thin layer chromatography (TLC) (Figures 2 and 3). Conclusions: [F-18]FEONM synthesized and purified by HPLC with EtOH as eluent can increase its chemical purity and prevent possible contamination of toxic organic solvents.
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