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

L W Herman, A J Fischman, R G Tompkins, R N Hanson, C Byon, H W Strauss, D R Elmaleh

Index: Nucl. Med. Biol. 21(7) , 1005-10, (1994)

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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.