Efficient synthesis of 1-heterocyclic-3-aminopyrrolidinones

Abstract A novel two-step synthesis of optically active 3-aminopyrrolidinones is described. The route allows access to pyrrolidinones with heterocyclic functionality that is incompatible with known methodology, and affords the final products in good to excellent yield and high enantiomeric purity. The Mitsunobu cyclodehydration is shown to be an efficient method for the formation of a variety of γ-lactams.