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.
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页码：1977 / 1984
页数：8
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