Synthesis of 3H‐ and 2H4‐labelled versions of the hypoxia‐activated pre‐prodrug 2‐[(2‐bromoethyl)‐2,4‐dinitro‐6‐ [[[2‐(phosphonooxy)ethyl]amino]carbonyl]anilino]ethyl methanesulfonate (PR‐104)

Abstract 3H‐ and 2H4‐versions of the hypoxia‐activated pre‐prodrug PR‐104 [2‐[(2‐bromoethyl)‐2,4‐dinitro‐6‐[[[2‐(phosphonooxy)ethyl]amino]carbonyl]anilino]ethyl methanesulfonate], labelled in the ethylcarboxamide side chain, have been prepared, respectively, by [3H]NaBH4 reduction of a precursor late stage aldehyde, and by late stage incorporation of deuterium with 2‐amino[1,1,2,2‐2H4]ethanol.