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14 C-radiolabeling of a new steroidal antiandrogen with a C-18 angular methyl extension.
- Source :
-
Journal of labelled compounds & radiopharmaceuticals [J Labelled Comp Radiopharm] 2024 Jan; Vol. 67 (1), pp. 25-30. Date of Electronic Publication: 2023 Dec 08. - Publication Year :
- 2024
-
Abstract
- The synthesis of a <superscript>14</superscript> C-labeled C-18 functionalized steroid (as referred as EM-6798) that will serve as a probe for the research of novel antiandrogens has been accomplished. This radioactive steroid was obtained in nine steps by coupling racemic N-cyclohexyl-1-(3'-hydroxy[U- <superscript>14</superscript> C]phenyl)propylamine with protected 18-bromomethyl-3,17-androstenedione. Incorporation of the radiolabel on the C-18 side chain was achieved using commercially available 3-bromo[U- <superscript>14</superscript> C]phenol. Alkylation of N-cyclohexyl-1-(3'-hydroxy[U- <superscript>14</superscript> C]phenyl)propylamine with 3-ethylenedioxy-18-bromomethyl-3,17-androstenedione furnished after reduction and deprotection, [phenyl-U- <superscript>14</superscript> C]EM-6798 in a 20% overall yield from 3-bromo[U- <superscript>14</superscript> C]phenol at a specific activity of 156 μCi/mg with 97.9% radiochemical purity as determined by HPLC.<br /> (© 2023 John Wiley & Sons, Ltd.)
- Subjects :
- Steroids
Phenols
Phenol
Propylamines
Androstenedione
Androgen Antagonists
Subjects
Details
- Language :
- English
- ISSN :
- 1099-1344
- Volume :
- 67
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Journal of labelled compounds & radiopharmaceuticals
- Publication Type :
- Academic Journal
- Accession number :
- 38066721
- Full Text :
- https://doi.org/10.1002/jlcr.4074