Recent Developments in the Synthetic Routes Towards Biologically Important Diarylpyrimidines (DAPYs)

Abstract Diarylpyrimidines (DAPYs) are privileged heteroaromatic scaffolds that have garnered significant interest in medicinal chemistry because of their wide range of biological activities, especially as HIV 1 non‐nucleoside reverse transcriptase inhibitors (NNRTIs), anticancer agents, and antimicrobial candidates. Many synthetic methods have been developed over the last 25 years (2000–2025) to access DAPY structural variants with improved pharmacological potential. These methods include nucleophilic substitutions, multicomponent reactions, palladium‐catalyzed couplings, and one‐pot green approaches. In contrast to previous studies, the current work not only compiles the existing solutions but also critically assesses their cost‐effectiveness, scalability, and adherence with green chemistry principles. Furthermore, it also emphasizes the biological potential of DAPYs as hybrid scaffolds for multitarget drug design. The comprehensive approach of this review is to provide a valuable and complete resource for synthetic and medicinal chemists in the development of next‐generation diarylpyrimidine derivatives.