Three‐Component Synthesis of 3‐(Arylsulfonyl)benzothiophenes Using Acetic Acid as a Quencher for Methyl Radical‐Mediated Side Reactions

Abstract A one‐pot, three‐component synthesis of 3‐(arylsulfonyl)benzothiophenes was developed. The reaction did not require any catalysts or additives. The desired products were obtained via an intramolecular radical cyclization. Acetic acid was employed as the solvent and a quencher for side reactions involving methyl radicals. Moreover, inexpensive potassium metabisulfite was used as a sulfur dioxide surrogate. This process provides more opportunities for synthesizing benzothiophene derivatives, which are found in many bioactive compounds. magnified image