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Synthesis of carbon-14 and tritiated steroidal 5α-reductase inhibitors

✍ Scribed by Arthur Y. L. Shu; J. Richard Heys


Publisher
John Wiley and Sons
Year
1994
Tongue
French
Weight
414 KB
Volume
34
Category
Article
ISSN
0022-2135

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✦ Synopsis


Abstract

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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