Chemistry. The first synthetic route to the pyrrolo [4, 3, 2-delisoquinoline system (Scheme I) involved an internal Mannich reaction of 4-aminomethylindole (1) 2 or 4- methylaminomethylindole (2) s with aliphatic or aromatic aldehydes to afford a series of 3- substituted and 3, 4-disubstituted 1, 3, 4, 5-tetrahydropyrrolo [4, 3, 2-de] isoquinolines