Synthesis of Biginelli Compounds using Microwave-Assisted Methods

Abstract

Biginelli adducts, also known as dihydropyrimidin-2(1H)-ones/-thiones (DHMPs), exhibit versatile biological activities. Among them, monastrol has gained significant popularity as an inhibitor of kinesin-5 (Eg5), a motor protein crucial for spindle bipolarity. The inhibitory effect of monastrol on Eg5 accounts for its promising anticancer properties, along with its well-established role as an anti-inflammatory agent and calcium channel inhibitor. Since its first report in 1893, the Biginelli reaction has been extensively studied from various angles, including the scope of reagents used, the incorporation or omission of catalysts and solvents, and the application of innovative techniques like mechanochemical and ultrasonic reactors. Among these methods, microwave irradiation (MWI) has shown remarkable promise, aligning with the principles of green chemistry by offering solvent-free conditions, eco-friendly catalysts, and accelerated reaction times, ultimately leading to higher yields with a reduced environmental impact. In this mini-review, we shed light on the literature surrounding the synthesis of Biginelli adducts using MWI and highlight how this heating method can significantly enhance the preparation of this important class of bioactive compounds. By exploring the benefits of MWI, we aim to contribute to the advancement of greener and more efficient synthetic routes for bioactive substances.