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A novel synthesis of [2-14C]2,5-dichloropyrimidine

✍ Scribed by Scott B. Tran; Brad D. Maxwell; Hong Wu; Samuel J. Bonacorsi Jr.

Publisher
John Wiley and Sons
Year
2011
Tongue
French
Weight
182 KB
Volume
54
Category
Article
ISSN
0022-2135

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✦ Synopsis

[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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