The Pd-catalyzed intramolecular α-arylation of α-amino acid esters is described. Starting fromreadily available amino acids, the synthesis of a variety of isoindolines and tetrahydroisoquinolinecarboxylic acid esters has been accomplished. Additionally, fused tricyclic systems can be efficientlyprepared from cyclic amino acid esters. Reaction conditions have been found that allow the use oftert-butyl ester and N-(benzyloxycarbonyl) protecting groups.