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A sequential post-transformation of Ugi four-component reaction/ nucleophilic substitution was developed for the synthesis of spiro-β-lactampyrroloquinolines. This method involves the Ugi-4CR of 2-chloro-3-formyl quinolines 1a−h, amines 2a−d, 2-chloroacetic acid 3, and isocyanides 4a, 4b for the synthesis of versatile precursors 5a−v. The Ugi adducts were intramolecularly cyclized under basic conditions through the sequential nucleophilic aromatic substitution (S N Ar)/second-order nucleophilic substitution (S N 2) reaction to give spiro-β-lactam-pyrroloquinoline scaffolds 6a−t. This approach is an efficient method for the synthesis of fused bioactive heterocyclic backbones containing quinoline, pyrrolidone, and β-lactam with high bond-forming efficiency.