Scott B. Tran, B. Maxwell, Hongui Wu
Nov 1, 2011
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Influential Citations
3
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Journal
Journal of Labelled Compounds and Radiopharmaceuticals
Abstract
[2-14 C]2,5-dichloropyrimidine is a useful reagent for labeling biologically active compounds for use in hepatocyte transport studies, protein covalent binding, and metabolic profiling. This paper describes a novel five-step synthesis of [2-14 C]2,5-dichloropyrimidine from readily available [14C]urea by way of a boronic acid intermediate. A total of 4.34 mCi of [2-14 C]2,5-dichloropyrimidine was obtained with a specific activity of 226.0 μCi/mg (33.7 mCi/mmol). The radiochemical purity was 95.8%, and the overall radiochemical yield was 22% based on 20 mCi of [14C]urea starting material. Copyright © 2011 John Wiley & Sons, Ltd.