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Copper‐Mediated Aminoquinoline‐Directed Radiofluorination of Aromatic C−H Bonds with K 18 F
Author(s) -
Lee So Jeong,
Makaravage Katarina J.,
Brooks Allen F.,
Scott Peter J. H.,
Sanford Melanie S.
Publication year - 2019
Publication title -
angewandte chemie
Language(s) - English
Resource type - Journals
eISSN - 1521-3757
pISSN - 0044-8249
DOI - 10.1002/ange.201812701
Subject(s) - chemistry , copper , combinatorial chemistry , carboxylic acid , functional group , medicinal chemistry , stereochemistry , organic chemistry , polymer
A Cu‐mediated ortho ‐C−H radiofluorination of aromatic carboxylic acids that are protected as 8‐aminoquinoline benzamides is described. The method uses K 18 F and is compatible with a wide range of functional groups. The reaction is showcased in the high specific activity automated synthesis of the RARβ2 agonist [ 18 F]AC261066.