title: New automated synthesis of [18F]FP-CIT with base amount control affording high and stable radiochemical yield: a 1.5-year production report.
abstract: We describe new [(18)F]Fluoropropylcarbomethoxyiodophenyl-nor-tropane ([(18)F]FP-CIT) automatic preparation method by (1) using 2-methyl-2-butanol as [(18)F]fluorination solvent, (2) base amount control to minimize side reaction and (3) salt elution method to elute trapped [(18)F]fluoride. We developed manual synthesis procedures for automatic synthesis application. In this manual synthesis, we trapped [(18)F]F(-) on ion exchange cartridge and eluted with 0.2 M potassium methanesulfonate solution. We have [(18)F]fluorination at 100°C with 2-methyl-2-butanol as protic solvent for [(18)F]fluorination. After high-performance liquid chromatography analysis, we have 69.3±3.2% of [(18)F]F(-) incorporation ratio on the manual synthesis and applied these conditions to automatic preparation with GE TracerLab FX module. After setting-up of automatic synthesis and quality control procedures for clinical procedures, we have routine production of [(18)F]FP-CIT with 86.9±9.5 GBq/2.5 ml of [(18)F]F(-) as initial radioactivity and have 192 productions for 1.5 year. We have 42.5±10.9% of decay corrected radiochemical yields and they were satisfied all quality control procedures and stability to 6 h. New [(18)F]FP-CIT automatic preparation method showed high and reliable radiochemical yield and we could have enough >35 patient doses of [(18)F]FP-CIT from one production.
authors.affiliation: Department of Nuclear Medicine, Asan Medical Center, University of Ulsan College of Medicine, Songpa-gu, Seoul 138-736, South Korea.
authors.forename: Sang Ju
authors.initials: SJ
authors.lastname: Lee
authors.forename: Seung Jun
authors.initials: SJ
authors.lastname: Oh
authors.forename: Woo Yeon
authors.initials: WY
authors.lastname: Moon
authors.forename: Moon Seok
authors.initials: MS
authors.lastname: Choi
authors.forename: Jae Seung
authors.initials: JS
authors.lastname: Kim
authors.forename: Dae Yoon
authors.initials: DY
authors.lastname: Chi
authors.forename: Dae Hyuk
authors.initials: DH
authors.lastname: Moon
authors.forename: Jin Sook
authors.initials: JS
authors.lastname: Ryu
mesh_terms: D001331:Automation; D054879:Halogenation; D006801:Humans; D011854:Radiochemistry / Q000379:methods*; D058028:Research Report; D014326:Tropanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000302:isolation & purification
chemical_list: D014326:Tropanes; C087552:2-carbomethoxy-8-(3-fluoropropyl)-3-(4-iodophenyl)tropane