A straightforward total synthesis of magallanesine 1 was accomplished from readily available isoquinolineacetate 14. This synthesis is emphasized by the following two points; i. the [1, 2]-Meisenheimer rearrangement of the azetidine N-oxide 22 for the preparation of azocine ring, ii. the Pd-catalyzed intramolecular Heck reaction of N-benzoylenaminone 38 for the construction of isoindoloazocine skeleton.