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Synthesis of 3‐[1 H ‐imidazol‐4‐yl]propyl 4‐[ 18 F]fluorobenzyl ether ([ 18 F]fluoroproxyfan): a potential radioligand for imaging histamine H 3 receptors
Author(s) -
Iwata Ren,
Horváth Géza,
Pascali Claudio,
Bogni A.,
Yanai Kazuhiko,
Kovács Zoltán,
Ido Tatsuo
Publication year - 2000
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 - 10.1002/1099-1344(200008)43:9<873::aid-jlcr371>3.0.co;2-a
Subject(s) - chemistry , radioligand , radiosynthesis , trifluoromethanesulfonate , bromide , ether , medicinal chemistry , yield (engineering) , alkylation , ligand (biochemistry) , amine gas treating , nucleophile , histamine , receptor , organic chemistry , in vivo , catalysis , biochemistry , pharmacology , medicine , materials science , microbiology and biotechnology , metallurgy , biology
3‐[1 H ‐Imidazol‐4‐yl]propyl 4‐fluorobenzyl ether (fluoroproxyfan), a potential histamine H 3 receptor ligand, was labelled with 18 F for clinical PET studies. The synthesis involved the O ‐alkylation of 3‐(1‐triphenylmethyl‐1 H ‐imidazol‐4‐yl)propanol with 4‐[ 18 F]fluorobenzyl bromide in the presence of silver triflate and a non‐nucleophilic amine base. 4‐[ 18 F]Fluoroproxyfan was obtained within 100 min from the end of bombardment (EOB) in 10% radiochemical yield (decay corrected to EOB) with a radiochemical purity >99% and a specific activity >150 GBq/μmol. Copyright © 2000 John Wiley & Sons, Ltd.