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A non-anhydrous, minimally basic protocol for the simplification of nucleophilic ^18^F-fluorination chemistry by Inkster, J. A. H.; Akurathi, V.; Sromek, A. W.; Chen, Y.; Neumeyer, J. L.; Packard, A. B. is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is A non-anhydrous, minimally basic protocol for the simplification of nucleophilic ^18^F-fluorination chemistry about?

## Abstract Fluorine-18 radiolabeling typically includes several conserved steps including elution of the [^18^F]fluoride from an anion exchange cartridge with a basic solution of K~2~CO~3~ or KHCO~3~ and Kryptofix 2.2.2. in mixture of acetonitrile and water followed by rigorous azeotropic drying to remove the water. In this work we describe an alternative “non-anhydrous, minimally basic” (“NAMB”) technique that simplifies the process and avoids the basic conditions that can sometimes limit the scope and efficiency of [^18^F]fluoride incorporation chemistry. In this approach, [^18^F]F^−^ is eluted from small (10–12 mg) anion-exchange cartridges with solutions of tetraethylammonium bicarbonate, perchlorate or tosylate in polar aprotic solvents containing 10–50% water. After dilution with additional aprotic solvent, these solutions are used directly in nucleophilic aromatic and aliphatic ^18^F-fluorination reactions, obviating the need for azeotropic drying. Perchlorate and tosylate are minimally basic anions that are nevertheless suitable for removal of [^18^F]F^-^ from the anion-exchange cartridge. As proof-of-principle, “NAMB” chemistry was utilized for the synthesis of the dopami

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Author
Inkster, J. A. H.; Akurathi, V.; Sromek, A. W.; Chen, Y.; Neumeyer, J. L.; Packard, A. B.
Publisher
Springer Science and Business Media LLC; London: Nature Publishing Group; [London]: Springer Nature; Nature Publishing Group; Society for Mining, Metallurgy and Exploration Inc.; Research Square; Springer Nature; Island Press (ISSN 2045-2322)
Published
2020
Language
EN
Field
Biochemistry, Genetics and Molecular Biology (Life Sciences)