Synthesis of 3-chloro-6-((4-(di-tert-butyl[(18)F]fluorosilyl)-benzyl)oxy)-1,2,4,5-tetrazine ([(18)F]SiFA-OTz) for rapid tetrazine-based (18)F-radiolabeling.

ABSTRACT

An efficient method to prepare the (18)F-labeled tetrazine-derivative [(18)F]-SiFA-OTz for bioorthogonal radiochemistry was developed. [(18)F]-SiFA-OTz can be synthesized with a radiochemical yield of 78 ± 5% within 25 min and can quantitatively react with a model strained dienophile, trans-cyclooctenol.