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1 article(s) from Maisonial, Aurélie

Use of 3-[¹⁸F]fluoropropanesulfonyl chloride as a prosthetic agent for the radiolabelling of amines: Investigation of precursor molecules, labelling conditions and enzymatic stability of the corresponding sulfonamides

Reik Löser,
Steffen Fischer,
Achim Hiller,
Martin Köckerling,
Uta Funke,
Aurélie Maisonial,
Peter Brust and
Jörg Steinbach

Beilstein J. Org. Chem. 2013, 9, 1002–1011, doi:10.3762/bjoc.9.115

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Figure 1: Selection of prosthetic agents for ¹⁸F-labelling via acylation.

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Scheme 1: Synthesis of radiofluorination precursors 3 and 4. Reagents and conditions: (a) KSCN, CH₃OH, reflux...

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Scheme 2: Synthesis of 3-fluoropropanesulfonamide 11 via intermediary 3-fluoropropanesulfonyl chloride (10). ...

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Scheme 3: Synthesis of 3-fluoropropanesulfonamides 12–18. Reagents and conditions: (a) triethylamine (TEA), CH...

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Figure 2: (A) View of the molecular structure of sulfonamide 18 with atom labelling scheme. Displacement elli...

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Figure 3: Dependence of the labelling yields of [¹⁸F]9 on the precursor amount. Reactions of tosylate 3 and n...

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Figure 4: Time course of the distillation of 3-[¹⁸F]fluoropropyl thiocyanate ([¹⁸F]9) in the argon stream. Fo...

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Scheme 4: Radiosynthesis of 3-[¹⁸F]fluoropropanesulfonamides [¹⁸F]11–[¹⁸F]18. Reagents and conditions: (a) [¹⁸...

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Figure 5: Radio-HPLC chromatograms for the reaction of [¹⁸F]10 with (A) 4-fluoroaniline in the absence and pr...

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Figure 6: Time course of the carboxylesterase-catalysed degradation of 3-fluoropropansulfonamide 17 (red) and...

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Published 27 May 2013

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Use of 3-[18F]fluoropropanesulfonyl chloride as a prosthetic agent for the radiolabelling of amines: Investigation of precursor molecules, labelling conditions and enzymatic stability of the corresponding sulfonamides

Use of 3-[¹⁸F]fluoropropanesulfonyl chloride as a prosthetic agent for the radiolabelling of amines: Investigation of precursor molecules, labelling conditions and enzymatic stability of the corresponding sulfonamides