SYNTHESIS OF POLYMER-BOUND 6-THIOLATOMERCURY AND 6-MERCURIC SULFONATEDOPA PRECURSORS AND THEIR HALODEMERCURATION REACTIVITY

Fluorodemercuration has the greatest utility for the preparation of 6- [F-18]DOPA, but requires separation from unreacted mercury precursor a nd other mercury-containing compounds. One approach is the development of a polymer-bound mercury precursor. Tn this study, polymer-bound 6- thiolatomercury and 6-mercuric sulfonate DOPA derivatives, and its mon omeric analogs were synthesized. Fluorodemercuration of monomeric anal og of mercuric sulfonate gave half the yield (14-15%) while iododemerc uration gave the same yield (38%) compared with a 6-mercuric trifluoro acetate protected DOPA. The mercuric sulfonate undergoes halodemercura tion, so polymer-bound halodemercuration precursors may be useful as p recursors of 6-[F-18]DOPA.