Copper-Catalyzed Directed Hydroindolation/Annulation Sequence of Alkynes with Indoles via Copper Carbenes

Guang Ma, Henan Agricultural University
Qiu-Yue Cui, Henan Agricultural University
Kua-Fei Wei, Henan Agricultural University
Xiao-Lei Jiang, Henan Agricultural University
Dong-Can Lv, Henan Agricultural University
Xiaoping Xue, Henan Agricultural University
Xiu-Hong Zhu, Henan Agricultural University
Guang-Xin Ru, Henan Agricultural University
Xinfeng Xie, Michigan Technological University
Wen-Bo Shen, Henan Agricultural University

Abstract

Described herein is an efficient copper-catalyzed tandem alkyne indolylcupration-initiated 1,2-indole migration/6π-electrocyclic reaction of allene-ynamides with indoles by the in situ-generated metal carbenes. This method allows the efficient synthesis of valuable indole-fused spirobenzo[]indole-cyclohexanes with high regio- and stereoselectivity. In addition, this reaction affords rapid access to the functionalized spirobenzo[]indole-cyclohexanes in the absence of indoles by a presumable 5-exo-dig cyclization/Friedel-Crafts alkylation via copper-containing all-carbon 1,4-dipoles.