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.
Keywords:
Biginelli reaction, microwave-assisted synthesis, green chemistry, MWI, bioactive substances, anticancer.
Graphical Abstract
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and
Ângelo de Fátima*
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