Based on the regioselective intermolecular Suzuki coupling and subsequent intramolecular Ullmann C–O coupling reactions, one-pot synthesis of benzo[4,5]thieno[3,2- b]benzofurans (BTBFs) was developed after optimization of the reaction conditions including catalysts, solvents, bases, ligands and reaction times. The one-pot reaction, with only 2 mol% Pd(PPh 3) 4 and 2 mol% copper( i) thiophene-2-carboxylate (CuTc) as the catalysts, K 3PO 4·3H 2O as the base and tert-butanol as the solvent, afforded moderate to good yields (up to 70%) for a variety of substrates.
Based on the regioselective intermolecular Suzuki coupling and subsequent intramolecular Ullmann coupling reactions, one-pot synthesis of benzo[4,5]thieno[3,2- b]benzofurans (BTBFs) has been developed.