A tandem Heck-aza-Michael addition protocol for the one-pot synthesis of isoindolines from unprotected amines.

A palladacycle-catalyzed tandem Heck-intramolecular aza-Michael reaction protocol has been developed for the one-pot synthesis of 1-substituted isoindolines from N-unprotected 2-bromobenzylamines and acrylates with high yields.