%0 Journal Article
%A Krapf, Philipp
%A Richarz, Raphael
%A Urusova, Elizaveta A.
%A Neumaier, Bernd
%A Zlatopolskiy, Boris D.
%T Seyferth-Gilbert Homologation as a Route to 18 F-Labeled Building Blocks: Preparation of Radiofluor­inated Phenylacetylenes and Their Application in PET Chemistry
%J European journal of organic chemistry
%V 2016
%N 3
%@ 1434-193X
%C Weinheim
%I Wiley-VCH Verl.
%M FZJ-2016-07768
%P 430 - 433
%D 2016
%X A convenient method for the preparation of hitherto unknown ([F-18]fluorophenyl)acetylenes ([F-18]FPAs) using the Seyferth-Gilbert homologation is reported. The novel building blocks were efficiently prepared from easily accessible [F-18]fluorobenzaldehydes by using the Bestmann-Ohira reagent. High radiochemical yields and excellent radiochemical purities were achieved within only 20 min of reaction time; 2- and 4-[F-18]FPAs were applied to prepare radiofluorinated heterocycles by using different cycloaddition and cross-coupling reactions. Additionally, these building blocks were used to prepare three novel PET tracers. Thus, an artificial radiofluorinated protected amino acid [F-18]10, a COX-2-specific ligand [F-18]14, and a PSMA-selective inhibitor [F-18]16 were obtained in high radiochemical yields.
%F PUB:(DE-HGF)16
%9 Journal Article
%U <Go to ISI:>//WOS:000368815700003
%R 10.1002/ejoc.201501377
%U https://juser.fz-juelich.de/record/825304