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Alternative synthesis for the preparation of 16 α-[18F]fluoroestradiol.
- Source :
-
Journal of Labelled Compounds & Radiopharmaceuticals . Oct2013, Vol. 56 Issue 12, p619-626. 8p. - Publication Year :
- 2013
-
Abstract
- We have developed a new precursor, 3,17 β-O-bis(methoxymethyl)-16 β-O-p-nitrobenzenesulfonylestriol (14c) of 16 α-[18F]fluoroestradiol ([18F]FES). Although we could not selectively protect the C17 alcohol in the presence of the C16 alcohol, we were able to prepare and chromatographically isolate the desired C16 TBDMS, C17,C3-dimethoxymethyl (diMOM) protected estriol derivative and convert into the ultimate fluorination precursor. The MOM protective group proved to be more quickly removed than the cyclic sulfate group. The di-MOM protective precursor at the C3 and C17 alcohols instead of a cyclic sulfate group shortened hydrolysis time. We prepared three different sulfonate precursors at C16 alcohol. After checking their reactivity in the [18F]fluorination step and considering the stability of the precursors, we obtained the best results with nosylate precursor 14c. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 03624803
- Volume :
- 56
- Issue :
- 12
- Database :
- Academic Search Index
- Journal :
- Journal of Labelled Compounds & Radiopharmaceuticals
- Publication Type :
- Academic Journal
- Accession number :
- 91930178
- Full Text :
- https://doi.org/10.1002/jlcr.3076