A practical and scalable synthesis of SR 142801, a tachykinin NK3 antagonist

被引：9

作者：

Chen, HG

Chung, FZ

Goel, OP

Johnson, D

Kesten, S

Knobelsdorf, J

Lee, HT

Rubin, JR

机构：

[1] Parke-Davis Pharmaceutical Res. Div., Warner-Lambert Company, Ann Arbor, MI 48105

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 05期

关键词：

D O I：

10.1016/S0960-894X(97)00064-4

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A practical and scalable total synthesis of tachykinin NK3 receptor antagonist SR 142801, (R)-N-[1-[3-[1-benzoyl-3-(3,4-dichlorophenyl)-3-piperidinyl]propyl]-4-phenyl-4-piperidinyl]-N-methyl acetamide 1 is described. The absolute configuration of the key intermediate 7 was determined by single crystal X-ray crystallography, on the basis of which, the absolute configuration of SR 142801 should be (R)-(+), instead of the recently reported (S)-(+).(1) (C) 1997 Elsevier Science Ltd.

引用

收藏

页码：555 / 560

页数：6

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