An efficient synthesis of the indole acetic acid metabolite of MK-0462

被引：15

作者：

Chen, CY ^{[1
]}

Lieberman, DR ^{[1
]}

Street, LJ ^{[1
]}

Guiblin, AR ^{[1
]}

Larsen, RD ^{[1
]}

Verhoeven, TR ^{[1
]}

机构：

[1] MERCK SHARP & DOHME LTD, RES LABS, HARLOW CM20 2QR, ESSEX, ENGLAND

来源：

SYNTHETIC COMMUNICATIONS | 1996年 / 26卷 / 10期

关键词：

D O I：

10.1080/00397919608003552

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A palladium-catalyzed coupling of iodoaniline 2 with bis-TES propargyl alcohol 3 gives indole-3-methanol 4b in 72% yield. Displacement of the hydroxy group of 4b by sodium cyanide followed by hydrolysis of the cyano group and desilylation provides the indole acetic acid metabolite, L-749,335 (1), of the 5-HT1D receptor agonist MK-0462.

引用

页码：1977 / 1984

页数：8

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