Rapid Electrophilic 211At‐Astatination of Trimethylgermyl Arenes

Abstract

AbstractA set of 211At‐astatoarenes were synthesized from corresponding trimethylgermyl arenes with an average radiochemical conversion (RCC) of ca. 50 % for electron‐rich and approx. 70 % in case of electron‐deficient arenes. 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 trimethylgermyl 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).