7014-88-2Relevant academic research and scientific papers
Synthesis and SAR of highly potent and selective dopamine D 3-receptor antagonists: 1H-Pyrimidin-2-one derivatives
Geneste, Herve,Backfisch, Gisela,Braje, Wilfried,Delzer, Juergen,Haupt, Andreas,Hutchins, Charles W.,King, Linda L.,Kling, Andreas,Teschendorf, Hans-Juergen,Unger, Liliane,Wernet, Wolfgang
, p. 490 - 494 (2006)
The synthesis and SAR of novel highly potent and selective dopamine D 3-receptor antagonists based on a 1H-pyrimidin-2-one scaffold are described. A-690344 antagonized PD 128907-induced huddling deficits in rat (ED50 6.1 mg/kg po), a social interaction paradigm.
PYRIMIDIN-2-ONE COMPOUNDS AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS
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Page 102, (2010/02/08)
The invention relates to pyrimidin-2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula: A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X-Y can also jointly represent C=CH, C=CH-CH2 or CH-CH=CH; R1 and R 2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents. The invention also relates to the use of compounds of formula (I), and their tautomers, derivatives and pharmacologically acceptable acid addition salts for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor ligands.
A convenient synthesis of masked β-ketoaldehydes by the controlled addition of nucleophiles to (trimethylsilyl)ethynyl ketones
Bromidge,Entwistle,Goldstein,Orlek
, p. 487 - 494 (2007/10/02)
The controlled addition of nucleophiles to (trimethylsilyl)ethynyl ketones provides a facile route to β-ketoacetals, β-alkoxy-α,β-unsaturated ketones or vinylogous amides depending on the choice of reaction conditions.
