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Facile synthesis of 2‐deoxy‐2‐[ 18 F]fluorosorbitol using sodium borohydride on aluminum oxide
Author(s) -
Hasegawa Koki,
Koshino Kazuhiro,
Higuchi Takahiro
Publication year - 2021
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3887
Subject(s) - sodium borohydride , chemistry , reagent , yield (engineering) , borohydride , radiosynthesis , nuclear chemistry , organic chemistry , materials science , nuclear medicine , catalysis , medicine , metallurgy , positron emission tomography
2‐Deoxy‐2‐[ 18 F]fluorosorbitol ( 18 F‐FDS) has become increasingly useful in functional renal imaging. FDS is synthesized by the one‐step reduction of 2‐deoxy‐2‐[ 18 F]fluoroglucose ( 18 F‐FDG). To develop a more simple and rapid procedure for 18 F‐FDS synthesis, we examined reduction reactions with solid‐supported NaBH 4 . Synthetic yields using BH 4 –IRA400 (polymer‐based matrix) and NaBH 4 –Al 2 O 3 (clay‐based matrix) as solid‐supported reagents were compared. NaBH 4 –Al 2 O 3 was found to be far superior to BH 4 –IRA400 in the FDG reduction reaction. IRA 400 was not suitable for this reaction because it adsorbs FDG, in addition to glucose, with no FDS synthesized when using BH 4 –IRA400. By contrast, NaBH 4 –Al 2 O 3 only required a filtration as workup, affording FDS in 90% yield after a total of 10 min. NaBH 4 on alumina was readily consumed in the reaction within 1 min, regardless of the amount used, by simply stirring with a vortex mixer. Complicated procedures, such as microwave irradiation, were not necessary. This simple operation will allow kit formulation and is suitable for radiosynthesis. In conclusion, clay‐supported reagents showed low absorption and were time saving, which are highly compatible with 18 F‐FDS synthesis.