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Beilstein J. Org. Chem. 2013, 9, 1002–1011, doi:10.3762/bjoc.9.115
Graphical Abstract
Figure 1: Selection of prosthetic agents for 18F-labelling via acylation.
Scheme 1: Synthesis of radiofluorination precursors 3 and 4. Reagents and conditions: (a) KSCN, CH3OH, reflux...
Scheme 2: Synthesis of 3-fluoropropanesulfonamide 11 via intermediary 3-fluoropropanesulfonyl chloride (10). ...
Scheme 3: Synthesis of 3-fluoropropanesulfonamides 12–18. Reagents and conditions: (a) triethylamine (TEA), CH...
Figure 2: (A) View of the molecular structure of sulfonamide 18 with atom labelling scheme. Displacement elli...
Figure 3: Dependence of the labelling yields of [18F]9 on the precursor amount. Reactions of tosylate 3 and n...
Figure 4: Time course of the distillation of 3-[18F]fluoropropyl thiocyanate ([18F]9) in the argon stream. Fo...
Scheme 4: Radiosynthesis of 3-[18F]fluoropropanesulfonamides [18F]11–[18F]18. Reagents and conditions: (a) [18...
Figure 5: Radio-HPLC chromatograms for the reaction of [18F]10 with (A) 4-fluoroaniline in the absence and pr...
Figure 6: Time course of the carboxylesterase-catalysed degradation of 3-fluoropropansulfonamide 17 (red) and...