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Synthesis of high specific activity 80m Br and 123 I labeled 5‐halodeoxyuridines and other 80m Br compounds for the study of auger electron toxicity
Author(s) -
Mease Rc,
Gatley Sj,
Friedman Am
Publication year - 1991
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.2580290405
Subject(s) - chemistry , yield (engineering) , sulfuric acid , radiochemistry , auger effect , nuclear chemistry , electron , inorganic chemistry , nuclear physics , materials science , metallurgy , physics
Convenient preparations of 80m Br and 123 I‐labeled 5‐halodeoxyuridines, required for basic investigations of Auger electron radiotoxicity, are described. These radioactive thymidine analogs were synthesized from deoxyuridine, radiohalide and N‐chlorosuccinimide in dilute sulfuric acid. Yields were 50–60% for 80m Br and 60–70% for 123 I. Apparent specific radioactivities (based on UV absorption under the radioactive HPLC peaks) were 150–550 Ci/mmol and over 2000 Ci/mmol for 80m Br and 123 I, respectively. 5‐[ 80m Br]bromouracil was produced in 89% yield when uracil was used. [ 80m Br]Bromoantipyrine was produced in higher yield and specific activity using peroxyacetic acid, rather than N‐chlorosuccinimide as oxidant (90% and 4,000 Ci/mmol versus 50% and 2000 Ci/mmol).