An Intramolecular Minisci Reaction in Aqueous Media Using Langlois’ Reagent

Abstract

A trifluoromethylpyridylation of unactivated alkenes in aqueous solution under open air is reported. This process allows the incorporation of trifluoromethyl and the construction of pyridines annulated to saturated cycles via an intramolecular Minisci reaction using Langlois’ reagent (CF₃SO₂Na) as a trifluoromethyl source. Extrusion of air from the reaction is not required. A broad functional group tolerance is observed. A series of five-, six-, and seven-membered cycles are obtained, exhibiting great potential application in the preparation of diversified pyridines.