Copper-Catalyzed N-Arylation/Hydroamin(d)ation Domino Synthesis of Indoles and its Application to the Preparation of a Chek1/KDR Kinase Inhibitor Pharmacophore

被引：83

作者：

Ackermann, Lutz ^{[1
]}

Barfuesser, Sebastian ^{[1
]}

Potukuchi, Harish K. ^{[1
]}

机构：

[1] Univ Gottingen, Inst Organ & Biomol Chem, D-37077 Gottingen, Germany

来源：

ADVANCED SYNTHESIS & CATALYSIS | 2009年 / 351卷 / 7-8期

关键词：

amination; arylation; catalysis; copper; hydroamination; indoles; ENDOTHELIAL GROWTH-FACTOR; N BOND FORMATION; C-N; EFFICIENT SYNTHESIS; REGIOSELECTIVE SYNTHESIS; 2-SUBSTITUTED INDOLES; REACTION SEQUENCE; COUPLING REACTION; ARYL HALIDES; ALKYNES;

D O I：

10.1002/adsc.200900004

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Inexpensive copper catalysts allow for efficient syntheses of N-aryl-, N-acyl-, or N-H-(aza)indoles starting from ortho-alkynylbromoarenes. The broad scope of this domino N-arylation/hydroamin(d)ation process is highlighted by the synthesis of highly functionalized indoles, as well as of a Chek1/KDR inhibitor pharmacophore.

引用

页码：1064 / 1072

页数：9

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