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Copper-Mediated Aminoquinoline-Directed Radiofluorination of Aromatic C-H Bonds with K18 F.

ABSTRACT: A Cu-mediated ortho-C-H radiofluorination of aromatic carboxylic acids that are protected as 8-aminoquinoline benzamides is described. The method uses K18 F and is compatible with a wide range of functional groups. The reaction is showcased in the high specific activity automated synthesis of the RAR?2 agonist [18 F]AC261066.

SUBMITTER: Lee SJ

PROVIDER: S-EPMC6476334 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature

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Copper-Mediated Aminoquinoline-Directed Radiofluorination of Aromatic C-H Bonds with K18 F.

Lee So Jeong SJ Makaravage Katarina J KJ Brooks Allen F AF Scott Peter J H PJH Sanford Melanie S MS

Angewandte Chemie (International ed. in English) 20190118 10

A Cu-mediated ortho-C-H radiofluorination of aromatic carboxylic acids that are protected as 8-aminoquinoline benzamides is described. The method uses K18 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. ...[more]

PMID: 30605563

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