Fused isoquinoline derivatives

Abstract

Abstract Fused isoquinoline derivatives of the general formula <IMAGE> (I) wherein: A is a divalent radical selected from the groups <IMAGE> wherein R3 and R4 each independently represents hydrogen, alkyl,, alkenyl, cycloalkyl, aryl, aralkyl, aralkenyl, cycloalkyl-alkyl or, taken together with the adjacent double bond, represent a cycloalkene containing from 5 to 8 carbon atoms or an aromatic nucleus; R5 represents hydrogen, hydroxyl, alkyl, alkenyl, cycloalkyl, aryl, aralkyl, aralkenyl or cycloalkyl-alkyl; Y is =O, =S or =NH; X is -O-, -S- or -NR6- wherein R6 represents hydrogen, alkyl, cycloalkyl, aryl, aralkyl or cycloalkyl-alkyl; R1 and R2 each independently represents hydrogen, alkyl, phenyl, cycloalkyl, alkoxy, alkenyloxy, methylenedioxy, cycloalkoxy, halo or di-alkylamino or, taken together with the adjacent carbon atoms of the benzene ring, form a cycloalkenyl group containing 5 or 6 carbon atoms or an aromatic nucleus fused on the benzene ring. The compounds are essentially prepared through thermal cyclization of a compound of the formula <IMAGE> (V) wherein A, X, Y, R1 and R2 have the same meanings given before, with the proviso that R1 and R2 cannot simultaneously occupy both the ortho positions, B represents hydrogen, R represents an -OR7 or -NR8R9 radical wherein R7 is alkyl, aryl or aralkyl and R8 and R9 each independently represents hydrogen, alkyl, aryl, aralkyl, or taken together with the adjacent nitrogen atom represent a heterocyclic saturated radical of 5 or 6 atoms which may contain a further hetero-atom selected from oxygen and nitrogen, or the symbols B and R taken together represent a further bond between the adjacent carbon and nitrogen atoms.

Inventors

• 👤 Giorgio Winters
• 👤 Nunzio DiMola

Bibliographic Details