Synthesis of a [18F]fluorobenzothiazole as potential amyloid imaging agent

  title={Synthesis of a [18F]fluorobenzothiazole as potential amyloid imaging agent},
  author={U. E. C. Berndt and Christian Stanetty and T. Wanek and C. Kuntner and J. Stanek and M. Berger and Martin Bauer and G. Henriksen and Hans-Juergen Wester and H. Kvaternik and P. Angelberger and C. Noe},
  journal={Journal of Labelled Compounds and Radiopharmaceuticals},
  • U. E. C. Berndt, Christian Stanetty, +9 authors C. Noe
  • Published 2008
  • Chemistry
  • Journal of Labelled Compounds and Radiopharmaceuticals
  • This study describes the synthesis of a fluoroethylated derivative of [N-methyl-11C]2-(4′-methylaminophenyl)-6-hydroxybenzothiazole ([11C]6-OH-BTA-1; Pittsburgh Compound B (PIB)), an already established amyloid imaging agent. The [11C]methylamino group of [11C]6-OH-BTA-1 was formally replaced by a fluoroethyl group in a cold synthesis via N-alkylation of N-Boc-2-(4′-aminophenyl)-6-(methoxyethoxymethoxy)benzothiazole with fluoroethyl tosylate. Subsequent deprotection gave the target compound 2… CONTINUE READING
    15 Citations

    Figures from this paper

    Synthesis and evaluation of 18F-fluoroethylated benzothiazole derivatives for in vivo imaging of amyloid plaques in Alzheimer's disease.
    • 13
    Radiolabeling of protected tryptophan with [18F]fluoromethyl tosylate: Formation of [18F]fluoromethyl ester of tryptophan instead of 1-N-[18F]fluoromethyl tryptophan methylester.
    AZD2184: a radioligand for sensitive detection of β‐amyloid deposits
    • 106
    Small Molecule-Assisted PET: Approaches to Imaging of Conformational Diseases of the Brain
    • 1
    • PDF
    Radiolabeled bioactive benzoheterocycles for imaging β-amyloid plaques in Alzheimer's disease.
    • Y. Yang, M. Cui
    • Chemistry, Medicine
    • European journal of medicinal chemistry
    • 2014
    • 27


    Radioiodinated styrylbenzenes and thioflavins as probes for amyloid aggregates.
    • 185
    Novel benzofuran derivatives for PET imaging of beta-amyloid plaques in Alzheimer's disease brains.
    • 84
    • PDF