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Synthesis of carbon‐14 and tritiated steroidal 5α‐reductase inhibitors
Author(s) -
Shu Arthur Y. L.,
Heys J. Richard
Publication year - 1994
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580340702
Subject(s) - chemistry , carbon 14 , tritium , tritiated water , 5 alpha reductase inhibitor , radiochemistry , biochemistry , organic chemistry , medicine , finasteride , prostate , physics , quantum mechanics , nuclear physics , cancer
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.