A reliable and efficient synthesis of SR 142801

被引：14

作者：

Giardina, GAM ^{[1
]}

Grugni, M ^{[1
]}

Rigolio, R ^{[1
]}

Vassallo, M ^{[1
]}

Erhard, K ^{[1
]}

Farina, C ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,DEPT MED CHEM,KING OF PRUSSIA,PA 19406

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 19期

关键词：

D O I：

10.1016/0960-894X(96)00419-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A convenient synthesis of the potent human NK-3 receptor antagonist SR 142801, (S)-(+)-N-{{3-[1-benzoyl-3-(3,4-dichlorophenyl)piperidin-3-yl]prop-1-yl}-4-phenylpiperidin-4-yl}-N-methylacetamide [(S)-(+)(15)], is described. Improvements over the previously reported procedure are the preparation of the intermediate 5 via the novel imide 3 and subsequent reaction with the nucleophile 14, which reacts, regioselectively, at the endocyclic nitrogen. Copyright (C) 1996 Elsevier Science Ltd

引用

页码：2307 / 2310

页数：4

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