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Synthesis of 18F-labelled biphenyls via SUZUKI cross-coupling with 4-[18F]fluoroiodobenzene

✍ Scribed by Björn Steiniger; Frank R. Wuest

Publisher
John Wiley and Sons
Year
2006
Tongue
French
Weight
147 KB
Volume
49
Category
Article
ISSN
0022-2135

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✦ Synopsis

The Suzuki reaction of organoboron compounds with 4-[ 18 F]fluoroiodobenzene has been developed as a novel radiolabelling technique in 18 F chemistry. The crosscoupling reaction of p-tolylboronic acid with 4-[ 18 F]fluoroiodobenzene was used to screen different palladium complexes, bases and solvents. Optimized reaction conditions (Pd 2 (dba) 3 , Cs 2 CO 3 , acetonitrile, 608C for 5 min) were further applied to the synthesis of various 18 F-labelled biphenyls bearing different functional groups. The reaction proceeded in excellent radiochemical yields of up to 94% within 5 min while showing good compatibility to many functional groups.

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