Regioselective C7 sulfinylation of 4-aminoindoles with sulfinates

Abstract

The regioselective C7-H sulfinylation of 4-aminoindoles was achieved by exploiting the para-directing ability of the amino group. This transformation utilizes readily available sulfinates as versatile sulfinyl sources, allowing facile installation of structurally diverse sulfoxide motifs at the C7 position. In addition to aryl/alkyl sulfinates, trifluoromethyl sulfinate is also viable.