Palladium-Catalyzed Direct 2-Alkylation of Indoles by Norbornene-Mediated Regioselective Cascade C-H Activation

被引:285
|
作者
Jiao, Lei
Bach, Thorsten [1 ]
机构
[1] Tech Univ Munich, Lehrstuhl Organ Chem 1, D-85747 Garching, Germany
关键词
ELECTRON-WITHDRAWING SUBSTITUENTS; DIRECT ARYLATION; PROTECTING GROUP; FUNCTIONALIZATION; ALKENYLATION; PYRROLES; OLEFINS; ROUTE; ALKYL; SELECTIVITY;
D O I
10.1021/ja2055066
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
A palladium-catalyzed direct 2-alkylation reaction of free N-H indoles has been developed. This reaction relies on a norbornene-mediated cascade C-H activation process at the indole ring, which features high regioselectivity and excellent functional group, tolerance. The reaction represents the first example for a generally applicable, direct C-H alkylation of indole at the 2-position.
引用
收藏
页码:12990 / 12993
页数:4
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