One-step synthesis of benzo[b]thiophenes by aryne reaction with alkynyl sulfides

Abstract

An aryne reaction with alkynyl sulfides affording benzo[b]thiophenes is disclosed. A wide range of 3-substituted benzothiophenes were synthesized from easily available o-silylaryl triflates and alkynyl sulfides in a one-step intermolecular manner. The synthesis of diverse multisubstituted benzothiophene derivatives involving a pentacyclic compound was achieved by virtue of the good functional group tolerance and versatile C2 functionalizations.