Construction of Benzothiophene or Benzothiopheno[2,3-e]azepinedione Derivatives via Three-Component Domino or One-Pot Sequences.

An efficient three-component domino or one-pot strategy has been developed for the synthesis of medicinally important benzothiophene and benzothiopheno[2,3-e]azepinedione derivatives for the first time. Amine-promoted selective cleavage of C-S bond of thioisatin is the key step in this process. The reported methodology benefits from environmentally friendly solvent (H2O), wide substrate scope, good functional group tolerance, and high reaction yields.