Synthesis of high specific activity 80mBr and 123I labeled 5-halodeoxyuridines and other 80mBr compounds for the study of auger electron toxicity
✍ Scribed by Rc Mease; Sj Gatley; Am Friedman
- Publisher
- John Wiley and Sons
- Year
- 1991
- Tongue
- French
- Weight
- 458 KB
- Volume
- 29
- Category
- Article
- ISSN
- 0022-2135
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✦ Synopsis
Abstract
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).