This title appears in the Scientific Report :
2016
Please use the identifier:
http://dx.doi.org/10.1002/ejoc.201501377 in citations.
Seyferth-Gilbert Homologation as a Route to 18 F-Labeled Building Blocks: Preparation of Radiofluorinated Phenylacetylenes and Their Application in PET Chemistry
Seyferth-Gilbert Homologation as a Route to 18 F-Labeled Building Blocks: Preparation of Radiofluorinated Phenylacetylenes and Their Application in PET Chemistry
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...
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Personal Name(s): | Krapf, Philipp |
---|---|
Richarz, Raphael / Urusova, Elizaveta A. / Neumaier, Bernd (Corresponding author) / Zlatopolskiy, Boris D. | |
Contributing Institute: |
Nuklearchemie; INM-5 |
Published in: | European journal of organic chemistry, 2016 (2016) 3, S. 430 - 433 |
Imprint: |
Weinheim
Wiley-VCH Verl.
2016
|
DOI: |
10.1002/ejoc.201501377 |
Document Type: |
Journal Article |
Research Program: |
Neuroimaging |
Publikationsportal JuSER |
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. |