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A novel synthesis of [2‐ 14 C]2,5‐dichloropyrimidine
Author(s) -
Tran Scott B.,
Maxwell Brad D.,
Wu Hong,
Bonacorsi Samuel J.
Publication year - 2011
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.1940
Subject(s) - chemistry , urea , boronic acid , specific activity , yield (engineering) , reagent , covalent bond , chemical synthesis , radiochemistry , combinatorial chemistry , organic chemistry , biochemistry , in vitro , enzyme , metallurgy , materials science
[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 [ 14 C]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 [ 14 C]urea starting material. Copyright © 2011 John Wiley & Sons, Ltd.
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