An overview of the most recent strategies for the construction of the pyrrolidine-2,3-dione platform, along with strategies toward its MedChem-relevant derivatives, is provided in this compilation. The microreview focuses on nonfunctionalized in positions 4 and 5 derivatives rather than well-reported 4-CO2R and 4-COR ones. The examples reported herein are arranged in three principal categories: assembly of the pyrrolidine-2,3-dione core, its functionalization, and the construction of sophisticated 3D chiral carcasses with high medicinal prospects based on the core. The summary includes works published within a period from 2020 to 2024.
