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Improved synthesis of pure [18F]fluoro-compounds for PET studies from bromo-compounds
Toshihiro Takahashi1, Takashi Mizuno, Tatsuo Ido
1Radioisotope Center, Niigata University, Asahimachi-dori 1-757, Niigata 951-8510, Japan. takatosi@med.niigata-u.ac.jp
Abstract:
For preparing [18F]labeled compounds free from bromo-compounds for PET (positron emission tomography) studies, we propose the following two processes in which no separation is needed between the fluoro-compound and bromo-compound : (1). the bromo-compound is first converted into O-tosylate, which is then [18F]fluorinated; and (2). after [18F]fluorination of the bromo-compound, its excess is converted into an easily separable compound, e.g., phthalimide-compound. Direct tosylation with silver tosylate was effected in 65-85% yield for most commercial bromo-compounds, and with potassium phthalimide, the bromo-compounds in cold run were converted easily into phthalimide-compounds in 84-90% yield.