The synthesis of 4, 5-dihydropyrrolo [2, la] isoquinolines is reported. A key intermediate in the synthesis of 8-methoxy-4, 5-dihydropyrrolo [2, lu] isoquinolines, 6-hydroxy-l, 2, 3, 4- tetrahydroisoquinoline-l-carboxylic acid (6), was prepared by using a regiospecific phenolic cyclization reaction. The P388 lymphocytic activity is reported for l, 2-bis (hydroxymethy)-5, 6- dihydro-8-methoxy-3-methylpyrrolo [2, 1-a] isoquinoline bis (isopropy1carbamate)(1 la), 1, ...