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Synthesis of polymer-bound 6-thiolatomercury and 6-mercuric sulfonate DOPA precursors and their halodemercuration
K Kawai1, M A Channing, D O Kiesewetter
1Department of Radiopharmaceutical Chemistry, Faculty of Pharmaceutical Sciences, Science University of Tokyo, Japan.
Abstract:
Fluorodemercuration has the greatest utility for the preparation of 6-[18F]DOPA, but requires separation from unreacted mercury precursor and other mercury-containing compounds. One approach is the development of a polymer-bound mercury precursor. In this study, polymer-bound 6-thiolatomercury and 6-mercuric sulfonate DOPA derivatives, and its monomeric analogs were synthesized. Fluorodemercuration of monomeric analog of mercuric sulfonate gave half the yield (14-15%) while iododemercuration gave the same yield (38%) compared with a 6-mercuric trifluoroacetate protected DOPA. The mercuric sulfonate undergoes halodemercuration, so polymer-bound halodemercuration precursors may be useful as precursors of 6-[18F]DOPA.