Synthesis of carbon‐14 and tritiated steroidal 5α‐reductase inhibitors
1994; Wiley; Volume: 34; Issue: 7 Linguagem: Inglês
10.1002/jlcr.2580340702
ISSN1099-1344
AutoresArthur Y. L. Shu, J. Richard Heys,
Tópico(s)Pharmacogenetics and Drug Metabolism
ResumoAbstract 17β‐[N‐(1,1‐Dimethylethyl)carbamoyl]androsta‐3,5‐diene‐4‐ 14 C‐3‐carboxylic acid ([ 14 C]SK&F 105657) was prepared via a three‐step sequence (t‐butyl amidation, triflation and carbomethoxylation) starting from androst‐4‐en‐3‐one‐4‐ 14 C‐17β‐carboxylic acid. Its A‐ring aromatic analog 17β‐[N‐(1,1‐dimethylethyl)carbamoyl]estra‐1,3,5‐(10)‐triene‐3‐carboxylic acid (SK&F 105656) was labeled with tritium by means of iridium‐mediated exchange methodology.
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