• Title/Summary/Keyword: $[^{18}F]$Fluorocholine derivatives

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Synthesis of [18F]Fluorocholine Analogues as a Potential Imaging Agent for PET Studies

  • Yu, Kook-Hyun;Park, Jeong-Hoon;Yang, Seung-Dae
    • Bulletin of the Korean Chemical Society
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    • v.25 no.4
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    • pp.506-510
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    • 2004
  • There have been intensive studies concerning $[^{11}F]$choline ($[^{11}F]$methyldimethyl( ${\beta}$ -hydroxyethyl) ammonium) (1) which is known as a very effective tracer in imaging various human tumors localized in brain, lung, esophagus, rectum, prostate and urinary bladder using Positron Emission Tomography (PET) and there is increasing interest in $^{18}F$ labelled choline (2) and proved to be useful to visualize prostate cancer. We have prepared six $^{18}F$ labelled alkyl choline derivatives (3a-3c, 4a-4c) from ditosylated and dibrominated alkanes in moderate yields. The six alkyl tosylate or bromate ammonium salts have been synthesized as precursors. Radiofluorination was achieved by the treatment of precursors with $^{18}F$ - in the presence of Kryptofix-2.2.2.. The labeling yields varied ranging from 7 to 25%.