Open AccessCopper-Mediated Radiofluorination of Arylstannanes with [18F]KF
Author(s) -
Katarina J. Makaravage,
Allen F. Brooks,
Andrew V. Mossine,
Melanie S. Sanford,
Peter J. H. Scott
Publication year - 2016
Publication title -
organic letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.94
H-Index - 239
eISSN - 1523-7060
pISSN - 1523-7052
DOI - 10.1021/acs.orglett.6b02911
Subject(s) - chemistry , aryl , nucleophile , reagent , copper , combinatorial chemistry , organic chemistry , catalysis , alkyl
A copper-mediated nucleophilic radiofluorination of aryl- and vinylstannanes with [ 18 F]KF is described. This method is fast, uses commercially available reagents, and is compatible with both electron-rich and electron-deficient arene substrates. This method has been applied to the manual synthesis of a variety of clinically relevant radiotracers including protected [ 18 F]F-phenylalanine and [ 18 F]F-DOPA. In addition, an automated synthesis of [ 18 F]MPPF is demonstrated that delivers a clinically validated dose of 200 ± 20 mCi with a high specific activity of 2400 ± 900 Ci/mmol.
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