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钯催化2-溴代或2-氯代苯胺与内炔烃的首例区域选择性吲哚化反应:一种合成2,3-二取代吲哚的新方法。

The first regioselective palladium-catalyzed indolization of 2-bromo- or 2-chloroanilines with internal alkynes: a new approach to 2,3-disubstituted indoles.

作者信息

Shen Ming, Li Guisheng, Lu Bruce Z, Hossain Azad, Roschangar Frank, Farina Vittorio, Senanayake Chris H

机构信息

Department of Chemical Development, Boehringer-Ingelheim Pharmaceuticals, Inc., 800 East Leigh Street, Suite 205, Richmond, Virginia 23219, USA.

出版信息

Org Lett. 2004 Oct 28;6(22):4129-32. doi: 10.1021/ol048114t.

Abstract

[reaction: see text] The first practical and economical process for synthesis of 2,3-disubstituted indole compounds has been developed with high regioselectivity by palladium-catalyzed indolization of 2-bromo- or chloroanilines and their derivatives with internal alkynes.

摘要

[反应:见正文] 已开发出首个实用且经济的合成2,3-二取代吲哚化合物的方法,该方法通过钯催化2-溴代或氯代苯胺及其衍生物与内炔烃进行吲哚化反应,具有高区域选择性。

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