2‐[(4‐[^18^F]Fluorobenzoyloxy)methyl]‐1,4‐naphthalenedione ([^18^F]**1**) was synthesised as a putative hypoxia imaging agent from 2‐hydroxymethyl 1,4‐naphthoquinone (**7**) and 4‐[^18^F]fluorobenzoic acid ([^18^F]**8**) using dicyclohexyl carbodiimide (DCC) to activate [^18^F]**8**. This coupling r
Microwave-assisted cyclocondensation of 1,2-diaminobenzene with [4-18F]fluorobenzoic acid: microwave synthesis of 2-([4-18F]fluorophenyl) benzimidazole
✍ Scribed by Gareth Getvoldsen; Anna Fredriksson; Nils Elander; Sharon Stone-Elander
- Publisher
- John Wiley and Sons
- Year
- 2004
- Tongue
- French
- Weight
- 99 KB
- Volume
- 47
- Category
- Article
- ISSN
- 0022-2135
- DOI
- 10.1002/jlcr.807
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✦ Synopsis
Abstract
The synthesis of 2‐([4‐^18^F]fluorophenyl)benzimidazole, which has potential to be used as a building block for many endogenous and pharmaceutical compounds, is reported. A range of solvents and catalysts as well as conventional and microwave heating have been investigated to optimise the reaction conditions. The cyclocondensation of 1,2‐diaminobenzene with radiolabelled [4‐^18^F]fluorobenzoic acid in neat methanesulphonic and polyphosphoric acids under microwave heating led rapidly to the cyclised phenylbenzimidazole. Copyright © 2004 John Wiley & Sons, Ltd.
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