Synthesis of 3-[1H-imidazol-4-yl]propyl 4-[18F]fluorobenzyl ether ([18F]fluoroproxyfan): a potential radioligand for imaging histamine H3 receptors

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公開日
2000-01-01
DOI
  • 10.1002/1099-1344(200008)43:9<873::aid-jlcr371>3.0.co;2-a
  • 10.1002/1099-1344(200008)43:9<873::aid-jlcr371>3.3.co;2-1
公開者
Wiley

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説明

3-[1H-Imidazol-4-yl]propyl 4-fluorobenzyl ether (fluoroproxyfan), a potential histamine H 3 receptor ligand, was labeled with 18 F for clinical PET studies. The synthesis involved the O-alkylation of 3-(1-triphenylmethyl-1H-imidazol-4-yl)propanol with 4-[ 18 F]fluorobenzyl bromide in the presence of silver triflate and a non-nucleophilic amine base. 4-[18F]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.

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