What question did this study set out to answer?

The aim is to develop a reproducible method for the radiofluorination of aryl halides using a sequential approach.

May 10, 2026Chemical Science0 citationsOpen Access

18 F-Labelling of (Hetero)aryl Halides via Sequential Miyaura Borylation/Copper-Mediated Radiofluorination

ANAbdias N. NoelUniversity of Michigan SGSamuel G. GrecoUniversity of Michigan MHMami HorikawaUniversity of Michigan

Key Points

The aim is to develop a reproducible method for the radiofluorination of aryl halides using a sequential approach.
Utilized a sequential Miyaura borylation and copper-mediated radiofluorination approach.
Targeted various heteroaryl iodide, bromide, and chloride substrates with palladium catalysis.
Successfully achieved radiofluorination with over 85% yield for several substrates.
Demonstrated broad applicability across different (hetero)aryl halide structures.

Abstract

This Article describes the development of a mild, general, and highly reproducible method for the radiofluorination of (hetero)aryl iodide, bromide, and chloride substrates. This transformation proceeds via sequential Pd-catalysed Miyaura...

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