Synthesis of [18 F]Fluoroform with High Molar Activity

Autor:	Anna Pees, Albert D. Windhorst, Maria J. W. D. Vosjan, Danielle J. Vugts, Vincent Tadino
Rok vydání:	2020
Předmět:	Molar chemistry.chemical_compound Fluoroform Chemistry Reagent Organic Chemistry Low density Isotopologue Pet imaging Physical and Theoretical Chemistry Isotope dilution Fluoride Combinatorial chemistry
Zdroj:	European Journal of Organic Chemistry. 2020:1177-1185
ISSN:	1434-193X
DOI:	10.1002/ejoc.202000056
Popis:	Fluoroform is an interesting motif for the isotopologue labelling of biologically active compounds with fluorine-18 for PET imaging. However, so far the building block [18F]fluoroform and consequently the [18F]trifluoromethylated products suffered from low molar activities ranging from 0.1 to 30 GBq/µmol due to isotopic dilution under the strongly basic standard radiofluorination conditions. In this article the synthesis of high molar activity [18F]fluoroform is described. By implementing a recently reported novel radiofluorination reagent, [18F]triflyl fluoride, the concentration of base-cryptand complex in the reaction could be reduced 100-fold compared to standard radiofluorination conditions and molar activities close to 100 GBq/µmol (at end of [18F]fluoroform synthesis) could be obtained, enabling the imaging of low density receptors. Furthermore, an automated procedure was developed on the commercially available NEPTIS® perform synthesizer to provide access of high molar activity [18F]fluoroform to other PET centres.
Databáze:	OpenAIRE
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