Indium(III) Chloride-Catalyzed One-Pot Synthesis of Dihydropyrimidinones by a Three-Component Coupling of 1,3-Dicarbonyl Compounds, Aldehydes, and Urea: An Improved Procedure for the Biginelli Reaction

2000 ◽  
Vol 65 (19) ◽  
pp. 6270-6272 ◽  
Author(s):  
Brindaban C. Ranu ◽  
Alakananda Hajra ◽  
Umasish Jana
Keyword(s):  
Biginelli Reaction ◽  
One Pot ◽  
Dicarbonyl Compounds ◽  
One Pot Synthesis ◽  
Three Component Coupling

scholarly journals One Pot Synthesis of Micromolar BACE-1 Inhibitors Based on the Dihydropyrimidinone Scaffold and Their Thia and Imino Analogues

Molecules ◽  
2020 ◽  
Vol 25 (18) ◽  
pp. 4152
Author(s):  
Jessica Bais ◽  
Fabio Benedetti ◽  
Federico Berti ◽  
Iole Cerminara ◽  
Sara Drioli ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Biginelli Reaction ◽  
Guanidine Hydrochloride ◽  
One Pot ◽  
Dicarbonyl Compounds ◽  
One Pot Synthesis ◽  
Bace 1

A library of dihydropyrimidinones was synthesized via a “one-pot” three component Biginelli reaction using different aldehydes in combination with β-dicarbonyl compounds and urea. Selected 2-thiooxo and 2-imino analogs were also obtained with the Biginelli reaction from thiourea and guanidine hydrochloride, respectively. The products were screened in vitro for their β-secretase inhibitory activity. The majority of the compounds resulted to be active, with IC50 in the range 100 nM–50 μM.

A Novel L-Proline Catalyzed Biginelli Reaction: One-Pot Synthesis of 3,4-Dihydropyrimidin-2(1H)-ones under Solvent-Free Conditions

2004 ◽  
Vol 33 (9) ◽  
pp. 1168-1169 ◽  
Author(s):  
J. S. Yadav ◽  
S. Praveen Kumar ◽  
G. Kondaji ◽  
R. Srinivasa Rao ◽  
K. Nagaiah
Keyword(s):  
Biginelli Reaction ◽  
Solvent Free ◽  
One Pot ◽  
One Pot Synthesis ◽  
Solvent Free Conditions

ChemInform Abstract: Three-Component Coupling of Acylphosphonates and Two Carbonyl Compounds Promoted by Low-Valent Samariums: One-Pot Synthesis of β-Hydroxyphosphonates.

ChemInform ◽  
2010 ◽  
Vol 31 (18) ◽  
pp. no-no
Author(s):  
Ken Takaki ◽  
Yuichiro Itono ◽  
Akihiro Nagafuji ◽  
Yoji Naito ◽  
Tetsuya Shishido ◽  
...  
Keyword(s):  
Carbonyl Compounds ◽  
One Pot ◽  
One Pot Synthesis ◽  
Low Valent ◽  
Three Component Coupling

Ca(NO3)2·4H2O-catalysed Biginelli Reaction: One-pot Synthesis of 1,2,3,4-Tetrahydropyrimidin-2-ones/pyrimidine-2-thiones under Solvent-free Conditions

2008 ◽  
Vol 26 (11) ◽  
pp. 2112-2116 ◽  
Author(s):  
Abdelmadjid DEBACHE ◽  
Raouf BOULCINA ◽  
Radia TAFER ◽  
Ali BELFAITAH ◽  
Salah RHOUATI ◽  
...  
Keyword(s):  
Biginelli Reaction ◽  
Solvent Free ◽  
One Pot ◽  
One Pot Synthesis ◽  
Solvent Free Conditions
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