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  • [Journal of Labelled Compounds and Radiopharmaceuticals] Design and synthesis of enantiopure 18F‐labelled [18F]trifluoromethyltryptophan from 2‐halotryptophan derivatives via copper(I)‐mediated [18F]trifluoromethylation and evaluation of its in vitro characterization for the serotonergic system imaging

    서울대 / 김호영, 정재민*

  • 출처
    Journal of Labelled Compounds and Radiopharmaceuticals
  • 등재일
    2019 May 28
  • 저널이슈번호
    Volume62, Issue9 July 2019 Pages 566-579
  • 내용

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    Abstract
    We synthesized [18F]trifluoromethyl‐l‐tryptophan ([18F]CF3‐l‐Trp) using Cu(I)‐mediated [18F]trifluoromethylation to image serotonergic system. Radiochemical yield was 6 ± 1.5% (n = 9), and radiochemical purity was over 99%. The molar activity was 0.44 to 0.76 GBq/μmol. [18F]CF3‐l‐Trp was stable for up to 6 hours in mouse and human sera at 37°C. Protein‐binding was 0.26 ± 0.03% and 0.34 ± 0.02% in human and mouse serum at 60 minutes, respectively. In conclusion, enantiopure [18F]CF3‐l‐Trp was synthesized as a feasible imaging agent for the serotonergic system.

     

    Ho Young Kim , Ji Youn Lee , Yun‐Sang Lee , Jae Min Jeong

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