13081-75-9Relevant academic research and scientific papers
Synthesis of 2,3-disubstituted 4-pyridone from a β-aminocarboxylate derivative and acetoacetate
Sobczak, Adam,Antkowiak, Wieslaw Z.
, p. 2993 - 3001 (2005)
The reaction of diethyl aminomethylenemalonate with ethyl acetoacetate proceeded, when catalyzed by anhydrous hydrogen chloride, toward a respectively substituted α- instead of γ-pyridone derivative formation, contrary to the literature report. Additionally, it was found that the amine used as a starting component in this reaction showed a great tendency to autocondensation under the influence of anhydrous hydrogen chloride to yield 5-ethoxycarbonyl-2- pyridone. The most convenient method to prepare 4-pyridone 2,3-disubstituted derivative appeared to be a three-step synthesis, starting from a chain enamine formation, which was subjected to cyclization, followed by oxidation of the last intermediate. The usefulness of the stepwise synthesis was demonstrated on the 3-ethoxycarbonyl-2-methyl-4-pyridone preparation as an example. Copyright Taylor & Francis, Inc.
NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A
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, (2013/02/28)
The present invention relates to novel carboxamide compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating or controlling medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders
