## Abstract Isothiocyanates have gained considerable attention for their role as potent chemopreventive agents. Sulforaphane, **1a** (SFN), a naturally occurring isothiocyanate, was isotopically labelled in five steps starting from 3‐(methylthio)‐1‐propanol (**2**)**.** Reacting **2** with tosyl ch
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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