Synthesis, characterization and radiolabeling of carborane-functionalized tetrazines for use in inverse electron demand Diels–Alder ligation reactions

Carborane-tetrazine derivatives were developed that can be used to enable boron clusters to bind specific targets in vivo using pretargeting strategies and bioorthogonal inverse electron demand Diels–Alder chemistry. Specifically, 1,12-dicarba-closo-dodecaborate-1-(4-(1,2,4,5-tetrazin-3-yl)phenyl)methanamide and 1,2-dicarba-closo-dodecaborate-1-(4-(1,2,4,5-tetrazin-3-yl)phenyl)methanamide were synthesized in 49% and 78% yield respectively, and …