Because of their enormous biological importance, 3,4-dihydropyrimidine-2(1H)-(thio)ones are gaining more and more attention every day. The traditional method of obtaining these scaffolds is through the Biginelli reaction, albeit there are some restrictions on the product diversity. Two key strategies have been developed to get around these limitations. The first one deals with altering the traditional Biginelli reaction components, while the second one discusses altering the Biginelli products after the fact. In this paper, both tactics have undergone substantial revision. Regarding the first, it was initially discussed how to modify one of the components. The modification of the keto ester counterpart was by far the most widely used strategy, and a wide range of different enolizablecarbonylic compounds were used. Additionally, changes in two or the three components were also described, extending the range of substitutes for the final dihydropyrimidines. In addition to these adjustments, decorating the final heterocyclic structure also benefited greatly by the usage of Biginelli adducts as a starting point for additional modifications.

Amalgamation, dihydropyrimidine, Biginelli