211 At-Astatination of Arenes Using Trimethylgermanyl Precursors.

A set of 211At-astatoarenes were synthesized from corresponding trimethylgermyl arenes with radiochemical conversions (RCCs) of up to 90%. Both electron rich and electron poor substrates were successfully radiolabeled at room temperature (RT) using relatively low precursor amounts (0.15 µmol/ 0.02 mL solvent (7.5 mM)). Ready access to ortho-, para- and meta- astatinated arenes was achievable. Optimized reaction conditions were successfully applied to label a poly (ADP-ribose) polymerase (PARP) inhibitor with a RCC of approx. 50%. We believe that trimethylgermanyl derivatives are a viable addition to the astatination precursor toolbox and facilitate astatination of arenes. The developed labeling method should easily be applicable for productions under good manufacturing practice (GMP).
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