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 synthesi zed and tested for F-18 exchange using tetrabutylammonium[F-18]fluorid e in DMSO, with microwave heating. A number of the compounds examined incorporated F-18 quickly and in high yield. Two compounds, pentafluor obenzaldehyde and 2,3,5,6-tetrafluorophenyl-pentafluorobenzoate, were used to label HSA in good yield. The methods produce low specific acti vity labelled proteins, but are fast. The yields are reasonable and th e reagents do not require a separate modification or activation step f or protein labelling.