SYNTHESIS OF C-14 AND TRITIATED STEROIDAL 5-ALPHA-REDUCTASE INHIBITORS

被引：13
|
作者：
SHU, AYL
HEYS, JR
机构：
[1] Radiochemistry Section, Department of Synthetic Chemistry, Smith Kline Beecham Pharmaceuticals, King of Prussia, Pennsylvania, 19406
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1994年 / 34卷 / 07期
关键词：
5-ALPHA-REDUCTASE INHIBITORS; RING-LABELED STEROIDS; IRIDIUM-MEDIATED TRITIUM EXCHANGE; AND H-3 NMR;
D O I：
10.1002/jlcr.2580340702
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
17 beta-[N-(1,1-Dimethylethyl)carbamoyl]androsta-3,5-diene-4-C-14-3-carboxylic acid ([C-14]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) 4C-17 beta-carboxylic acid. Its A-ring aromatic analog 17 beta-[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.
引用
收藏
页码：587 / 596
页数：10
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