THE SYNTHESIS OF A CONFORMATIONALLY RESTRICTED ANALOG OF THE ANTIMIGRAINE DRUG SUMATRIPTAN

被引：44

作者：

MACOR, JE

BLANK, DH

POST, RJ

RYAN, K

机构：

[1] Department of Medicinal Chemistry Central Research Division, Pfizer Inc, Groton

来源：

TETRAHEDRON LETTERS | 1992年 / 33卷 / 52期

关键词：

D O I：

10.1016/S0040-4039(00)74703-4

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The synthesis of 5-N-Methylaminosulfonylmethyl-3-(N-methylpyrrolidin-2-ylmethyl)indole (1), a conformationally restricted analog of the anti-migraine drug, sumatriptan, is described. To incorporate our novel stereogenic replacement for the aminoethyl sidechain in sumatriptan, a convergent synthesis of the 3,5-disubstituted indole (1) was employed which utilized an intramolecular Heck reaction as the cornerstone reaction.

引用

页码：8011 / 8014

页数：4

共 14 条

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