Original synthesis of radiolabeling precursors for batch and on resin one-step/late-stage radiofluorination of peptides

Chem Commun (Camb). 2020 Feb 25;56(16):2507-2510. doi: 10.1039/c9cc09434b.

Abstract

Radiolabeling of peptides with fluorine-18 is hurdled by their chemical sensitivity and complicated processes. Original triflyl-pyridine intermediates afforded ammonium precursors that were radiolabeled at low temperature. From that study, a generic tag has been designed to allow a simple one-step/late-stage radiolabelling of peptides. The strategy has been transposed to an automated "on-resin" radiolabelling.

MeSH terms

  • Fluorine Radioisotopes
  • Halogenation
  • Molecular Structure
  • Peptides / chemical synthesis*
  • Peptides / chemistry
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Resins, Synthetic / chemical synthesis*
  • Resins, Synthetic / chemistry
  • Temperature

Substances

  • Fluorine Radioisotopes
  • Peptides
  • Radiopharmaceuticals
  • Resins, Synthetic
  • Fluorine-18