TY - JOUR
T1 - Improved synthesis of pure [18F]fluoro-compounds for PET studies from bromo-compounds
AU - Takahashi, Toshihiro
AU - Mizuno, Takashi
AU - Ido, Tatsuo
AU - Iwata, Ren
AU - Watanabe, Ken Ichi
N1 - Funding Information:
The operation of the cyclotron by the members of the Cyclotron and Radioisotope Center is acknowledged and appreciated. Part of this study was presented at the Fifth Japan–China Joint Seminar on Radiopharmaceutical Chemistry, Sendai, Japan, 2000. This study was supported by a Grant-in-Aid (No. 08877314) for Scientific Research from the Ministry of Education, Science and Culture, Japan.
PY - 2003/5
Y1 - 2003/5
N2 - 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.
AB - 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.
KW - Bromo-compound
KW - O-tosyl-compound
KW - Potassium phthalimide-compound, PET study
KW - Silver tosylate
KW - [F]fluoro-compound
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U2 - 10.1016/S0969-8043(03)00053-8
DO - 10.1016/S0969-8043(03)00053-8
M3 - Article
C2 - 12735972
AN - SCOPUS:0038148162
VL - 58
SP - 557
EP - 566
JO - Applied Radiation and Isotopes
JF - Applied Radiation and Isotopes
SN - 0969-8043
IS - 5
ER -