Open AccessSynthesis of [18F]Arenes via the Copper-Mediated [18F]Fluorination of Boronic Acids
Author(s) -
Andrew V. Mossine,
Allen F. Brooks,
Katarina J. Makaravage,
Jason Miller,
Naoko Ichiishi,
Melanie S. Sanford,
Peter J. H. Scott
Publication year - 2015
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.5b02875
Subject(s) - chemistry , copper , aryl , combinatorial chemistry , functional group , stereochemistry , organic chemistry , alkyl , polymer
A copper-mediated radiofluorination of aryl- and vinylboronic acids with K(18)F is described. This method exhibits high functional group tolerance and is effective for the radiofluorination of a range of electron-deficient, -neutral, and -rich aryl-, heteroaryl-, and vinylboronic acids. This method has been applied to the synthesis of [(18)F]FPEB, a PET radiotracer for quantifying metabotropic glutamate 5 receptors.