HIGH SPECIFIC ACTIVITY-STEROIDS .2. MICROSCALE SYNTHESIS OF NORGESTREL-[9,11-H-3]

被引：4
|
作者：
HUANG, GT
MCCARTHY, KE
PARNES, H
机构：
[1] Institute of Organic Chemistry, Syntex Research, Palo Alto, California, 94303
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1992年 / 31卷 / 12期
关键词：
TRITIATED; 19-NONSTEROIDS; HIGH SPECIFIC ACTIVITY; NORGESTREL-[9,11-H-3;
D O I：
10.1002/jlcr.2580311206
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
The synthesis of the high specific activity (39 Ci/mmole) tritium labelled steroid norgestrel is described. A practical synthesis of the required substrate for tritium incorporation, 18-methyl-DELTA9(11)-estradiol-3-methyl ether (6), was developed from norgestrel itself. Following reduction with carrier-free tritium gas, microscale conditions were employed for the conversion of the resulting labelled intermediate (7) back to norgestrel-[9,11-H-3], including a selective in situ protection of the A-ring ketone of 19-norandrost-4-ene-3,17-dione (11).
引用
收藏
页码：995 / 1003
页数：9
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