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•Important mechanisms are briefly covered and the most plausible one highlighted.•Substrate variations have been show-cased.•Approaches to optically-enriched DHPMs are presented with biological activities.•Natural products with DHPM skeletons are discussed.•Applications of Biginelli reaction for the development of materials are presented.
Biginelli reaction involves acid-catalyzed one-pot synthesis of 3,4-dihydropyrimidin-2(1H)-ones (DHPMs) using easily-accessible starting materials, namely, aldehyde, active methylene compound and (thio)urea. DHPMs have stimulated resurgence of interest in the past two decades due to their wide ranging pharmacological activities and presence of diverse natural products. Presently, green approaches to asymmetric Biginelli reaction are being explored for bioactive chiral DHPMs. In materials chemistry, DHPMs are increasingly finding applications in the development of materials such as polymers, adhesives, fabric dyes, etc. In view of the ease with which the Biginelli reaction is conducted, many exciting prospects await for its exploitation in various fields.