THE USE OF PENTAFLUOROPHENYL DERIVATIVES FOR THE F-18 LABELING OF PROTEINS

A simple, one-step method for the radiolabelling of proteins with F-18 is described. A series of pentafluorophenyl derivatives were synthesized and tested for F-18 exchange using tetrabutylammonium[F-18]fluoride in DMSO, with microwave heating. A number of the compounds examined incorporated F-18 quickly and in high yield. Two compounds, pentafluorobenzaldehyde and 2,3,5,6-tetrafluorophenyl-pentafluorobenzoate, 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.