ABSTRACT The synthesis of 1-(4-aminophenyl)-4-methyl-7, 8-methylenedioxy-5 H-2, 3- benzodiazepine (GYKI 52466, 1), the prototype of a series of noncompetitive AMPA receptor antagonists, and its 3, 4-dihydroderivative (GYKI 52895, 2) is described. The title compounds have been prepared starting from safrole through a quite effective procedure.