Cu(I)-catalyzed cascade intramolecular cyclization of 2-propynol phenyl azides and diarylphosphine oxides for the synthesis of bisphosphorylated indole derivatives

The [Cu(OTf)](2).C6H6 catalyzed cascade intermolecular addition-intramolecular cyclization reaction of easily prepared 2-propynol phenyl azides and diarylphosphine oxides was developed. This novel reaction leads to simultaneous formation of one C-N and two C-P bonds in a single step to give bisphosphorylated indole derivatives under mild conditions in moderate to good yields. (C) 2018 Elsevier Ltd. All rights reserved.