Advances in Biginelli reaction: A comprehensive review

Abstract

The Biginelli reaction, a conventional three‐component reaction provides 3,4‐dihydropyrimidin‐2(1H)‐ones/thiones via one‐pot acid catalyzed cyclocondensation of an aldehyde, a β‐keto ester, and urea or thiourea. Dihydropyrimidones are well‐known scaffolds having a wide range of pharmacological activities. So far classical Biginelli reaction has witnessed several modification and studies are still continuing in this field to develop greener and efficient methodologies. In this review, we summarize the recent advances in Biginelli reaction covering literature from 2020 to 2023.

Synthesis and Antiproliferative Properties of Some Spirocyclic Pyrimidine Hydrazones

“…Based on these findings and in combination with our interest in anticancer agents [28][29][30][31] along with our previous research on pyrimidine-containing molecules, [32][33][34] we report, herein, a series of new hydrazone derivatives 4 a-l (Scheme 1) containing spirocyclic aminopyrimidine and aryl alkanesulfonate moieties. To access the starting compound, we used a Biginelli reaction which is an example of the multicomponent reaction [35] by which cyclohexanone, malononitrile and thiourea were reacted in one-pot process to produce the spirocyclic pyrimi-dine. Taking into account the paucity of literature reports dealing with either spirocyclic pyrimidines or aryl alkanesulfonates, we emphasize here that this is the first study dealing with the connection of aryl alkanesulfonates to spirocyclic pyrimidine via azomethine linker.…”