Radiochemical F-18-fluoroarylation of unsaturated alpha-, beta- and gamma-amino acids, application to a radiolabelled analogue of baclofen

Unsaturated alpha-, beta- and gamma-amino acids have been investigated as substrates for the reductive Meerwein arylation. Radical reactions of this type have been shown to be a valuable tool for the fast and efficient introduction of the 4-[F-18]fluorophenyl group into precursor molecules allowing...

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Bibliographic Details
Published inTetrahedron Vol. 64; no. 52; pp. 11846 - 11851
Main Authors Hoefling, Sarah B., Hultsch, Christina, Wester, Hans-Juergen, Heinrich, Markus R.
Format Journal Article
LanguageEnglish
Published OXFORD Elsevier 22.12.2008
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
POLAR
ARENEDIAZONIUM
RESOLUTION
CHEMISTRY
GABA
ALPHA,BETA-UNSATURATED CARBONYL-COMPOUNDS
SALTS
BINDING
(R)-BACLOFEN
PEPTIDE
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Summary:Unsaturated alpha-, beta- and gamma-amino acids have been investigated as substrates for the reductive Meerwein arylation. Radical reactions of this type have been shown to be a valuable tool for the fast and efficient introduction of the 4-[F-18]fluorophenyl group into precursor molecules allowing short-time syntheses of potential PET radiotracers, which would be more difficult to access by other methods. (C) 2008 Elsevier Ltd. All rights reserved.
ISSN:0040-4020
DOI:10.1016/j.tet.2008.07.117