14 C-radiolabeling of a new steroidal antiandrogen with a C-18 angular methyl extension.
J Labelled Comp Radiopharm
; 67(1): 25-30, 2024 Jan.
Article
in En
| MEDLINE
| ID: mdl-38066721
ABSTRACT
The synthesis of a 14 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-14 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-14 C]phenol. Alkylation of N-cyclohexyl-1-(3'-hydroxy[U-14 C]phenyl)propylamine with 3-ethylenedioxy-18-bromomethyl-3,17-androstenedione furnished after reduction and deprotection, [phenyl-U-14 C]EM-6798 in a 20% overall yield from 3-bromo[U-14 C]phenol at a specific activity of 156 µCi/mg with 97.9% radiochemical purity as determined by HPLC.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Androgen Antagonists
/
Androstenedione
Language:
En
Journal:
J Labelled Comp Radiopharm
Year:
2024
Document type:
Article
Affiliation country: