• Chemistry, Medicine
  • Published in
    Journal of labelled compounds…
    2017
  • DOI:10.1002/jlcr.3469

Efficient synthesis of [18 F]FPyME: A new approach for the preparation of maleimide-containing prosthetic groups for the conjugation with thiols.

@article{Cavani2017EfficientSO,
  title={Efficient synthesis of [18 F]FPyME: A new approach for the preparation of maleimide-containing prosthetic groups for the conjugation with thiols.},
  author={Melanie Cavani and Dirk Bier and Marcus H. Holschbach and Heinz H. Coenen},
  journal={Journal of labelled compounds & radiopharmaceuticals},
  year={2017},
  volume={60 1},
  pages={
          87-92
        }
}
An improved high yielding radiosynthesis of the known thiol-reactive maleimide-containing prosthetic group1-[3-(2-[18 F]fluoropyridine-3-yloxy)propyl]pyrrole-2,5-dione ([18 F]FPyME) is described. The target compound was obtained by a two-step one-pot procedure starting from a maleimide-containing nitro-precursor that was protected as a Diels-Alder adduct with 2,5-dimethylfurane. Nucleophilic radiofluorination followed by heat induced deprotection through a Retro Diels Alder reaction yielded… CONTINUE READING

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