Abstract: The Biginelli Reaction stands out as a highly versatile one-pot cyclocondensation process that effectively combines β-keto esters, urea, and aromatic aldehydes in the presence of a catalyst. This powerful reaction yields various 3,4-dihydro-2(H)-pyrimidinones (DHPMs), known for their significant pharmacological applications in synthetic and natural forms. In recent years, this reaction has been expertly refined to improve efficiency and reduce environmental impact. By employing a range of catalysts and green solvents, such as water, researchers achieve high yields of DHPMs in an environmentally friendly manner. In this review, we have thoroughly explored the literature on Biginelli reactions carried out under aqueous conditions, utilizing various reaction promoters, including catalysts, polymers, and enzymes, all in an eco-conscious way. The article encompasses the advantages of the use of ‘in water’ synthesis in various facets and highlights a sustainable pathway for the Biginelli reaction, facilitating the efficient synthesis of bioactive compounds while prioritizing environmental preservation.
Khanna et al. (Fri,) studied this question.