First preparation of enantiomerically pure sibutramine and its major metabolite, and determination of their absolute configuration by single crystal X-ray analysis

被引：23

作者：

Fang, QK

Senanayake, CH

Han, ZX

Morency, C

Grover, P

Malone, RE

Bulter, H

Wald, SA

Cameron, TS

机构：

[1] Sepracor Inc, Chem Proc Res & Dev, Marlborough, MA 01752 USA

[2] Dalhousie Univ, Dept Chem, Halifax, NS B3H 4J3, Canada

来源：

TETRAHEDRON-ASYMMETRY | 1999年 / 10卷 / 23期

关键词：

D O I：

10.1016/S0957-4166(99)00511-X

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Racemic sibutramine was resolved with dibenzoyl-D-tartaric acid, and the absolute stereochemistry of sibutramine was determined by single crystal X-ray crystallography of its dibenzoyl D-tartrate. The major active metabolite (desmethylsibutramine) was obtained by demethylation of sibutramine with DEAD. Enantiomeric purity of sibutramine was determined by HPLC on an Ultron ES-OVM column. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：4477 / 4480

页数：4

共 6 条

[1] THE PHARMACOLOGY OF SIBUTRAMINE HYDROCHLORIDE (BTS54524), A NEW ANTIDEPRESSANT WHICH INDUCES RAPID NORADRENERGIC DOWN-REGULATION [J].