Facile solid-phase construction of indole derivatives based on a traceless, activating sulfonyl linker

被引：184

作者：

Zhang, HC ^{[1
]}

Ye, H ^{[1
]}

Moretto, AF ^{[1
]}

Brumfield, KK ^{[1
]}

Maryanoff, BE ^{[1
]}

机构：

[1] RW Johnson Pharmaceut Res Inst, Drug Discovery, Spring House, PA 19477 USA

来源：

ORGANIC LETTERS | 2000年 / 2卷 / 01期

关键词：

D O I：

10.1021/ol991255o

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

[GRAPHICS] Palladium-mediated coupling/intramolecular indole cyclization of terminal alkynes with resin 8, followed by cleavage of the sulfonamide linkage, were executed under mild conditions to provide diverse indoles 10 in excellent yield and purity. This chemistry benefits from a dual activation process that derives from use of a traceless N-sulfonyl linker. Also, direct mercuration of 9 (X = H, R = 4-Me-C6H4), followed by palladium mediated coupling with methyl acrylate, efficiently provided I functionalized product 12.

引用

页码：89 / 92

页数：4

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