Environmentally friendly and regioselective C3-alkylation of indoles with alcohols through a hydrogen autotransfer strategy

Abstract

The direct alkylation of indoles using KOH and alcohols, as initial source of the electrophile, under solvent-free conditions is a safe and environmentally benign strategy for selective modification of these structures at the C3-position, without using hazardous and difficult to handle bromide or iodide derivatives or toxic and expensive transition metal catalysts. The protocol shows a broad scope, including halogenated indoles and secondary alcohols.