Efficient copper-catalyzed synthesis of C3-alkylated indoles from indoles and alcohols

A highly efficient copper(II) catalyst system for alkylation of indoles with alcohols via hydrogen borrowing method has been developed to afford C3-alkylated indoles in good to excellent yields. Cu(OAc)(2) in the combination with dppm ligand has been found to be the most suitable catalyst system for this alkylation reaction.

Automated summary

A highly efficient copper(II) catalyst system has been developed for alkylation of indoles with alcohols via hydrogen borrowing method, yielding C3-alkylated indoles in good to excellent yields. The combination of Cu(OAc)(2) with dppm ligand has been found to be the most suitable catalyst system for this alkylation reaction.