Shen Ming, Li Guisheng, Lu Bruce Z, Hossain Azad, Roschangar Frank, Farina Vittorio, Senanayake Chris H
Department of Chemical Development, Boehringer-Ingelheim Pharmaceuticals, Inc., 800 East Leigh Street, Suite 205, Richmond, Virginia 23219, USA.
Org Lett. 2004 Oct 28;6(22):4129-32. doi: 10.1021/ol048114t.
[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.
[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。