The title furoisoquinoline was synthesized by regioselective [4+2] cycloaddition between 5-bromo-2-methylbenzo[b]furan-4,7-dione (I) and 3-(tert-butyldimethylsilyloxy)-1-isopropoxy-2-aza-buta-1,3-diene (II), with simultaneous desilylation under the reaction conditions.