Since the last decade, the paradigm has been shifted to "Green Chemistry" to meet the challenges of sustainable development. It has become the quest and challenge for chemists to develop green reaction process without affecting their efficiency to reduce the environmental impact. Further, it is likely that the green chemistry trend will continue to grow over the next few decades. Interestingly, the Biginelli-scaffolds have shown promising value in drug development as they exhibit a wide spectrum of pharmacological activities. During the past years, copious research has been done on Biginelli-scaffolds and several reaction conditions were reported to ease the classical Biginelli-reaction.This book provides insights on green method for the synthesis of Biginelli-scaffolds by both microwave and conventional methods using sulfamicacid as a potential catalyst and further synthesis of 4-aryl-3,4-dihyropyrimidin-2(3H)-onesand biological screening for various pharmacological activities.