Synthesis of [1,2-(3)H]ethylamine hydrochloride and [(3)H]-labeled apadenoson for a human ADME study

Tritium-labeled [1,2-(3)H]ethylamine hydrochloride was prepared through a multiple-step sequence in high radioactive specificity. The labeled amine was isolated in high purity following cartridge filtration and used subsequently in the synthesis of [N-ethyl-1,2-(3)H]apadenoson, an adenosine A(2a) receptor agonist. The overall yield for this transformation was 56% and the radiochemical purity of the final product was greater than 99%.