The technology features a novel three-component ligand system that centers around a bis(tert-butyltriazolyl)methyl amine catalytic core, a customizable linker, and a fluorous tag. This unique assembly enables rapid reaction kinetics and high catalytic efficiency for Cu(I)-catalyzed azide-alkyne cycloaddition reactions. Its well-controlled synthesis process—including multistep conversion, click reactions, acid treatment, and reduction—yields a final structure that can be fine-tuned by adjusting the fluorous tag length and linker properties. By dramatically reducing copper toxicity, the system facilitates rapid removal of copper via solid-phase extraction and achieves high radiochemical purity even at nanomolar concentrations, making it particularly suitable for radiometal labeling in biomedical applications such as PET imaging.
Description
This technology is differentiated by its modular approach and superior performance over conventional Cu(I) ligands. The ability to quickly and selectively remove the metal catalyst addresses longstanding toxicity concerns while significantly enhancing reaction yields. Moreover, its adaptable design allows for customization of solubility and spatial configuration, making it versatile for a range of applications—from radiolabeling small peptides to imaging of antibodies—thus setting a new benchmark in both catalyst efficiency and bioconjugation strategies.
Applications
- Radiometal labeling for PET
- Rapid peptide radiolabeling
- Antibody radiolabeling imaging
- Bioconjugate diagnostic synthesis
Advantages
- Highly efficient catalysis from the bis(tert-butyltriazolyl)methyl amine core, boosting reaction speed.
- Rapid radiometal labeling (≈10 minutes) with high yield and radiochemical purity.
- Substantially reduced copper toxicity through fluorous tag-enabled removal via solid-phase extraction.
- Minimal copper transchelation, ensuring stability in sensitive radiopharmaceutical applications.
- Customizable linker design allows tuning of solubility and spatial configuration for diverse biomedical uses.
IP Status
https://patents.google.com/patent/US11167277B2
