Recent progress in synthetic strategies for novel β-lactams linked with five-membered heterocycles (N/O/S): advances in medicinal chemistry (2020–2025)

β-Lactam derivatives have inspired chemists to develop synthetic methods, given the prevalence of β-lactam scaffolds in numerous existing drugs. Recently, the incorporation of β-lactam derivatives into diverse heterocycles using novel pharmacophoric hybridization strategies has led to the development of compounds with significant medicinal applications. The five-membered heterocycles incorporating heteroatoms, such as nitrogen, oxygen, and sulfur, influence their chemical and biological properties. Advances in synthetic strategies, including transition metal catalysis, Staudinger cycloaddition, the Kinugasa reaction, halocyclization, and functionalization using available β-lactam drugs, have facilitated the construction of a variety of β-lactam scaffolds. This article presents an in-depth review of the latest methods for the synthesis of five-membered heterocycles (N/O/S) linked β-lactams from 2020–2025. This review aims to support researchers in designing and developing novel β-lactam linked with five-membered heterocycles (N/O/S) with enhanced therapeutic efficacy by delving into recent advances (2020–2025) in synthetic endeavors for β-lactams.