Synthesis method of 3,4-dihydropyrimidin-2-ketone compounds catalyzed by ionic liquid at room temperature
The present invention discloses a synthesis method of 3,4-dihydropyrimidin-2-ketone compounds catalyzed by ionic liquid at room temperature. Key technology is as follows: nano-silicon-loaded bronsted acid functional group ionic liquid is used as a catalys
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Paragraph 0028; 0048; 0049
(2017/07/06)
Identification and characterization of 4-aryl-3,4-dihydropyrimidin-2(1H)-ones as inhibitors of the fatty acid transporter FATP4
Several potent, cell permeable 4-aryl-dihydropyrimidinones have been identified as inhibitors of FATP4. Lipophilic ester substituents at the 5-position and substitution at the para-position (optimal groups being -NO2 and CF3) of the 4-aryl group led to active compounds. In two cases racemates were resolved and the S enantiomers shown to have higher potencies.
Solid-Phase Synthesis of Dihydropyrimidones via N-Acyliminium Ion-Based α-Ureidoalkylations
The synthesis of 4-aryl-2-(thioxo)oxo-3,4-dihydropyrimidine-5-carboxylic acids is reported using two orthogonal solid-phase variations of the Biginelli condensation. In the first method, polymer-bound β-ketoesters are treated with aromatic aldehydes and urea under acidic conditions. The transient N-acyliminium ion that is initially formed from the aldehyde and urea precursors, is then intercepted by the resin-bound β-ketoesters. In an alternative approach, resin-bound β-ketoesters are condensed with aldehydes and O-methylisourea under basic conditions. Both orthogonal condensation procedures provide fair to excellent overall yields of the desired target structures.
Valverde, Maria Garcia,Dallinger, Doris,Kappe, C. Oliver
p. 741 - 744
(2007/10/03)
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