Biginelli reaction beyond three-component limit: synthesis of functionalized pyrimidinones via a one-pot Biginelli-Pd mediated C–C coupling strategy

Synthesis, crystal structure and antibacterial studies of dihydropyrimidines and their regioselectively oxidized products

“…It is known that a lot of protocols were developed for performing Biginelli reaction, leading to the synthesis of H 2 Py with high yields under "green" conditions and simple work-up procedure. Using catalyst types such as I 2 /MWI, 67 Yb(PFO) 3 , 68 TMSCl/CAN, 69 [Hmim]HSO 4 -NaNO 3 , 70 CAN, 71 [3][4][5][6][7][8][9][10][11][12][13][14] it was not possible to perform a Biginelli reaction on the basis of all used aldehyde scaffolds, urea and methylacetoacetate. In addition to this, performing the synthesis in microwave reactor becomes more popular over the conventional method, due to the fact that microwave method increases speed, reproducibility and scalability of the reaction.…”

“…It is still in trend, due to the fact that this exible and multilateral tool allows construction of an astonishing class of compounds with a broad spectrum of application area, namely dihydropyrimidines (H 2 Py). [2][3][4][5][6][7][8] First of all, it must be mentioned that these marvelous compounds are important heterocyclic systems which play a crucial role as a building block of biomolecules such as DNA and RNA. 9 Among other applications of these amazing compounds, the synthesis and development of materials with novel optical properties, 10 design of polymers, 11 dyes 12 and adhesives 13 can be mentioned.…”

Novel alkynyl substituted 3,4-dihydropyrimidin-2(1H)-one derivatives as potential inhibitors of chorismate mutase

“…Thus, an overall four component reaction was developed involving a sequential phosphorous acid-mediated Biginelli followed by Cu-free Sonogashira or Heck or Suzuki reaction [26]. The use of elemental iodine on the other hand has been explored for successful Biginelli reaction earlier [27].…”

Combinatorial Chemistry Online

“…It is thought the methodology, will find wide application in combinatorial and diversity-oriented synthesis of dihydropyrimidones of potential pharmacological interest. 4 Parallel diversity-oriented synthesis of diverse 1-(1H-imidazol-1-yl)-1,2-dihydroisoquinolines via AgOTf-catalysed three-component reaction of 2-alkynylbenzaldehyde, amine, and imidazole has been described. This reaction works efficiently under mild conditions to generate a small library of imidazole-incorporated 1,2-dihydroisoquinolines.…”