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5-benzylpyrrolidine-2,4-dione 9 are versatile scaffolds with a unique structural feature responsible for the diversity of its biological importance. Over the past years, many researchers have reported the synthesis of various bio-active (S)-5-benzylpyrrolidine-2,4-dione derivatives due to their simplicity yet exhibiting promising bioactivities. This review focuses on the synthesis of core structure 9 and its derivatives based on the substitution at carbon-3 position of (S)-5-benzylpyrrolidine- 2,4-dione 9. This review also reported the effective method for the synthesis of core structure 9 with a 98% yield. Biological evaluations of various prepared derivatives by various researchers were described.