Indoles Synthesized from Amines via Copper Catalysis

被引：21

作者：

Besandre, Ronald ^{[1
]}

Jaimes, Miguel ^{[1
]}

May, Jeremy A. ^{[1
]}

机构：

[1] Univ Houston, Dept Chem, Houston, TX 77204 USA

来源：

ORGANIC LETTERS | 2013年 / 15卷 / 07期

关键词：

RECEPTOR-BINDING AFFINITIES; DEMANDING N-SUBSTITUENTS; ONE-POT SYNTHESIS; INTRAMOLECULAR CYCLIZATION; NUCLEOPHILIC-ADDITION; CYTOSTATIC ACTIVITY; CARBONYL-COMPOUNDS; MODULAR SYNTHESIS; ACTIVE COMPOUNDS; CROSS-COUPLINGS;

D O I：

10.1021/ol400444g

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

N-Substituted indoles are synthesized from primary amines through a tandem reaction sequence. Initial condensation of the amine with an alpha-(o-haloaryl)ketone or aldehyde is followed by intramolecular aryl amination catalyzed by CuI. A variety of anilines and alkyl amines, including those with significant steric demands, are converted to indoles in high yields and with varying indole substitution.

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收藏

页码：1666 / 1669

页数：4

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