Development of a 11C-labeled tetrazine for rapid tetrazine-trans-cyclooctene ligation

Tetrazine-trans-cyclooctene ligations are remarkably fast and selective reactions even at low micro-molar concentrations. In bioorthogonal radiochemistry, tools that enable conjugation of radioactive probes to pre-targeted vectors are of great interest. Herein, we describe the successful development of the first C-11-labelled tetrazine and its reaction with trans-cyclooctenol.