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

页码：119 / 125

页数：7

共 7 条

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[2]

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[4]

KOE BK, 1983, J PHARMACOL EXP THER, V226, P686

[5]

Kraay GM, 1930, RECL TRAV CHIM PAY-B, V49, P1082

[6]

RONFELD RA, COMMUNICATION

[7] NONTRICYCLIC ANTIDEPRESSANT AGENTS DERIVED FROM CIS-1-AMINO-4-ARYLTETRALIN AND TRANS-1-AMINO-4-ARYLTETRALIN [J].

WELCH, WM ;

KRASKA, AR ;

SARGES, R ;

KOE, BK .

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