The inverse electron-demand Diels-Alder reaction as a new methodology for the synthesis of 225Ac-labelled radioimmunoconjugates

The inverse electron-demand Diels-Alder reaction between tetra-zine (Tz) and trans-cyclooctene (TCO) facilitates the efficient radio-synthesis of Ac-225-labelled radioimmunoconjugates in a two-step method, outperforming conventional approaches based on isothio-cyanate couplings.