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Synthesis of 3 H‐ and 2 H 4 ‐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)
Author(s) -
Atwell Graham J.,
Denny William A.
Publication year - 2007
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.1147
Subject(s) - chemistry , prodrug , aldehyde , deuterium , ethanol , medicinal chemistry , stereochemistry , organic chemistry , catalysis , biochemistry , physics , quantum mechanics
3 H‐ and 2 H 4 ‐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 [ 3 H]NaBH 4 reduction of a precursor late stage aldehyde, and by late stage incorporation of deuterium with 2‐amino[1,1,2,2‐ 2 H 4 ]ethanol. Copyright © 2007 John Wiley & Sons, Ltd.