The use of pentafluorophenyl derivatives for the 18F labelling of proteins

Nucl Med Biol. 1994 Oct;21(7):1005-10. doi: 10.1016/0969-8051(94)90091-4.

Abstract

A simple, one-step method for the radiolabelling of proteins with 18F is described. A series of pentafluorophenyl derivatives were synthesized and tested for 18F exchange using tetrabutylammonium-[18F]fluoride in DMSO, with microwave heating. A number of the compounds examined incorporated 18F quickly and in high yield. Two compounds, pentafluorobenzaldehyde and 2,3,5,6-tetrafluorophenylpentafluorobenzoate, were used to label HSA in good yield. The methods produce low specific activity labelled proteins, but are fast. The yields are reasonable and the reagents do not require a separate modification or activation step for protein labelling.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Animals
  • Benzoates / chemistry*
  • Fluorine Radioisotopes / chemistry*
  • Fluorobenzenes / chemistry*
  • Isotope Labeling / methods*
  • Rats
  • Rats, Sprague-Dawley
  • Serum Albumin / chemistry
  • Serum Albumin / pharmacokinetics

Substances

  • 2,3,5,6-tetrafluoro 2,3,4,5,6-pentafluorobenzoate
  • Benzoates
  • Fluorine Radioisotopes
  • Fluorobenzenes
  • Serum Albumin
  • pentafluorobenzoic acid