Iron-Catalyzed Direct C3-Benzylation of Indoles with Benzyl Alcohols through Borrowing Hydrogen

• DOI: 10.1021/acs.joc.7b01603
• Publication Date: 2017-07-26T13:39:19Z
• Authors: Giovanni Di Gregorio; Michele Mari; Francesca Bartoccini; Giovanni Piersanti
• Keywords: Benzyl alcohol

We present the coupling of primary and secondary benzyl alcohols with indoles to form 3-benzylated H2O that is catalyzed, for first time, by a complex earth-abundant iron. This transformation accommodates variety substrates distinguished its operational simplicity, sustainability, high functional-group tolerance, amenability gram-scale synthesis. On basis preliminary experimental observations, we propose reaction proceeds through borrowing hydrogen process.