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Synthesis and hydrolytic stability of novel 3-[18F]fluoroethoxybis(1-methylethyl)silyl]propanamine-based prosthetic groups
- Source :
-
Journal of Fluorine Chemistry . Apr2011, Vol. 132 Issue 4, p250-257. 8p. - Publication Year :
- 2011
-
Abstract
- Abstract: Two new silicon-based prosthetic groups, derived from 3-[ethoxybis(1-methylethyl)silyl]propanamine, have been prepared in good yields. These silicon groups bearing an acid or an azide group were coupled to a model tripeptide (Leu-Gly-Gly) either through a classical amide bond formation or through “click chemistry” via the Huisgen cycloaddition. The radiolabelling with fluorine-18 by substitution of the ethoxy group at silicon has been carried out with success in 51–54% decay corrected radiochemical yields. Radiolabelled peptides were easily prepared by direct 18F-fluorination of the silicon-bearing tripeptide or by coupling the peptide with a radiolabelled silicon-based prosthetic group. Their stabilities in physiological medium were studied and proved poor. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 00221139
- Volume :
- 132
- Issue :
- 4
- Database :
- Academic Search Index
- Journal :
- Journal of Fluorine Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 59776775
- Full Text :
- https://doi.org/10.1016/j.jfluchem.2011.01.011