Application of Daugulis Copper-Catalyzed Direct Arylation to the Synthesis of 5-Aryl Benzotriazepines

被引：75

作者：

Yotphan, Sirilata

Bergman, Robert G. ^{[1
]}

Ellman, Jonathan A.

机构：

[1] Univ Calif Berkeley, Dept Chem, Berkeley, CA 94720 USA

来源：

ORGANIC LETTERS | 2009年 / 11卷 / 07期

关键词：

H BOND ACTIVATION; ANTAGONISTS; POTENT; FUNCTIONALIZATION; ALKENYLATION; QUINOLINES; INHIBITORS; DISCOVERY; PYRIDINES;

D O I：

10.1021/ol900103a

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A method for the direct arylation of benzotriazepines is reported, employing an aryl iodide as the coupling partner, copper iodide as the catalyst, and lithium tert-butoxide as the base. A variety of electron-rich, electron-poor, and sterically hindered aryl iodides are compatible with the reaction conditions. The arylation reaction can also be performed outside a glovebox in air without a significant decrease in yield. Furthermore, convenient microwave conditions for carrying out this transformation are reported.

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页码：1511 / 1514

页数：4

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