The pyrimidine nucleus plays an important role in designing the bioactive drugs which have abundant medicinal properties. Numerous synthetic methods have been available in literature to synthesize this nucleus. The synthesis of biologically significant dihydropyrimidinones (DHPMs) having a pyrimidine nucleus has been a subject of significant interest due to their prominent pharmacological potentials. The advanced synthetic pathways that provide shorter time duration, energy efficient approach, solvent free reaction conditions, and higher yields are still in the thought of researchers. In recent years, microwave and ultrasonic assisted synthesis methods have emerged as an alternative energy efficient source for the efficient and rapid generation of complex molecules, including DHPMs. This review provides a comprehensive reports of the recent advancements in microwave and ultrasonic assisted synthesis techniques for the preparation of DHPMs (2018–2023). It discusses the principles underlying microwave and ultrasonic irradiation and their application in organic synthesis. Various synthetic strategies used for the microwave and ultrasonic-assisted synthesis of DHPMs are elaborated in this. Moreover, paper also emphasizes the benefits of microwave and ultrasonic irradiation over conventional heating techniques, shorter reaction times, higher yields, and better selectivity. Mechanistic insights into the impact of microwave and ultrasonic irradiation on reaction kinetics and product formation are also discussed. The impact of microwave and ultrasonic irradiation on reaction kinetics and product generation is also examined from a mechanistic perspective. In summary, this review underscores the noteworthy contribution of microwave and ultrasonic aided synthetic methods to the progress of DHPM synthesis and points to future directions for research in this promising area.