SYNTHESIS OF 7-H-3-(1S,4S)-4-(3,4-DICHLOROPHENYL)-1,2,3,4-TETRAHYDRO-N-METHYL-L-NAPHTHALENAMINE HYDROCHLORIDE (7-H-3-SERTRALINE)

被引：3
|
作者：
WELCH, WM [1 ]
WILLIAMS, MT [1 ]
机构：
[1] PFIZER,CENT RES LABS,DEPT PROC RES & DEV,SANDWICH CT13 9MJ,KENT,ENGLAND
来源：
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1993年 / 33卷 / 02期
关键词：
H-3-SERTRALINE; H-3-CP-51,974-01; ANTIDEPRESSANT; 5-HT UPTAKE INHIBITOR;
D O I：
10.1002/jlcr.2580330206
中图分类号：
Q5 [生物化学];
学科分类号：
071010 ; 081704 ;
摘要：
The preparation of the title compound, a selective serotonin uptake inhibitor with antidepressant properties in man, is described. The preparation of the 7-bromo precursor via a stereoselective seven-step sequence from (1R)-7-bromo-1,2,3,4-tetrahydro-N-methyl-1-nephthalenamine is described. The radiochemical purity of the product obtained after reduction with tritium was greater than 99 % and the specific activity was 17.6 Ci/mM.
引用
收藏
页码：119 / 125
页数：7
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