一种构建高度取代吲哚的环化方法：酚类添加剂对酮烯醇盐芳基化反应成功的异常影响。
An annulative approach to highly substituted indoles: unusual effect of phenolic additives on the success of the arylation of ketone enolates.
作者信息
Rutherford Jennifer L, Rainka Matthew P, Buchwald Stephen L
机构信息
Department of Chemistry, Massachusetts Institute of Technology, Cambridge, Massachusetts 02139, USA.
出版信息
J Am Chem Soc. 2002 Dec 25;124(51):15168-9. doi: 10.1021/ja0288993.
A novel palladium-catalyzed arylation of ketone enolates with o-nitrohaloarenes was achieved through the addition of phenol additives. The mild reaction conditions employed allowed for the inclusion of a wide variety of functional groups in both substrates to be tolerated. The products of this reaction were then readily reductively cyclized to give highly substituted indoles in moderate to excellent overall yields.
通过添加苯酚添加剂，实现了一种新型的钯催化酮烯醇盐与邻硝基卤代芳烃的芳基化反应。所采用的温和反应条件使得两种底物中都能容纳多种官能团。然后，该反应的产物很容易进行还原环化，以中等至优异的总收率得到高度取代的吲哚。
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