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Palladium(II)-Catalyzed Tandem Cyclization/C–H Functionalization of Alkynes for the Synthesis of Functionalized Indoles

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posted on 19.10.2012, 00:00 by Xiao-Feng Xia, Ning Wang, Lu−Lu Zhang, Xian-Rong Song, Xue-Yuan Liu, Yong-Min Liang
A palladium-catalyzed tandem cyclization/C–H functionalization of two alkynes was accomplished to construct a series of polycyclic functionalized indoles. A range of internal alkynes bearing synthetically useful functional groups were tolerated. A good regioselectivity was observed when alkyl-substituted alkynes were introduced into the reaction system, and a single product was obtained. Molecular oxygen was used as the terminal oxidant in the approach, rendering the reaction more sustainable.