Journal Article

FZJ-2016-07768

http://join2-wiki.gsi.de/foswiki/pub/Main/Artwork/join2_logo100x88.png Seyferth-Gilbert Homologation as a Route to 18 F-Labeled Building Blocks: Preparation of Radiofluor­inated Phenylacetylenes and Their Application in PET Chemistry

Krapf, P.FZJ* ; Richarz, R.FZJ* ; Urusova, E. A. ; Neumaier, B. (Corresponding author)FZJ* ; Zlatopolskiy, B. D.

2016
Wiley-VCH Verl. Weinheim

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Please use a persistent id in citations: doi:10.1002/ejoc.201501377

Abstract: 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.

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Contributing Institute(s):

1. Nuklearchemie (INM-5)

Research Program(s):

1. 573 - Neuroimaging (POF3-573) (POF3-573)

Appears in the scientific report 2016

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Database coverage:
; Current Contents - Physical, Chemical and Earth Sciences ; IF < 5 ; JCR ; NCBI Molecular Biology Database ; SCOPUS ; Science Citation Index ; Science Citation Index Expanded ; Thomson Reuters Master Journal List ; Web of Science Core Collection

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