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- Title
<sup>18</sup>F‐Fluorination of a supported 2‐(aryl‐di‐tert‐butylsilyl)‐N‐methyl‐imidazole for indirect <sup>18</sup>F‐labeling of a V<sub>H</sub>H single‐variable domain.
- Authors
Steffann, Marine; Bluet, Guillaume; Roy, Sébastien; Aubert, Catherine; Fouquet, Eric; Hermange, Philippe
- Abstract
Anchoring an imidazole‐di‐tert‐butyl‐arylsilane possessing an azido group to a polystyrene resin provided a heterogeneous precursor that was radiolabeled easily using aqueous [18F]fluoride. After optimizing the conditions (i.e., using DMSO as solvent and heating at 160°C for 15 min), the desired [18F]fluorosilane was obtained in 24% radiochemical yield (RCY) and 78% radiochemical purity (RCP) using solid‐phase extraction as sole purification. Then, this compound was conjugated by strain‐promoted alkyne–azide cycloaddition to a model single‐variable domain possessing a cyclooctyne tag, yielding to the desired 18F‐labeled bioconjugate in 2% RCY and >95% RCP after purification by a size exclusion chromatography.
- Subjects
GEL permeation chromatography; RADIOCHEMICAL purification; AZIDO group; SOLID phase extraction
- Publication
Journal of Labelled Compounds & Radiopharmaceuticals, 2024, Vol 67, Issue 3, p104
- ISSN
0362-4803
- Publication type
Article
- DOI
10.1002/jlcr.4082