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Fast and efficient synthesis of 14C labelled benzonitriles and their corresponding acids

✍ Scribed by Søren Christian Schou


Publisher
John Wiley and Sons
Year
2009
Tongue
French
Weight
122 KB
Volume
52
Category
Article
ISSN
0022-2135

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✦ Synopsis


Abstract

^14^C‐Anthranilic acid has been prepared in a fast and efficient way in a two‐step reaction in 82% overall radiochemical yield. Thus, 2‐iodoaniline was transformed into 2‐amino‐[7‐^14^C]‐benzonitrile using a palladium catalyzed cyanation with zinc ^14^C‐cyanide. Subsequent basic hydrolysis of the cyano group afforded [7‐^14^C]‐anthranilic acid. The method was successfully applied to a benzophenone scaffold, 4‐iodophenol and 4‐iodobenzoic acid producing the corresponding carboxylic acids in good to excellent radiochemical yields (62–82%) and with high specific activity (1.94–1.98 GBq/mmol). Copyright © 2009 John Wiley & Sons, Ltd.


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