42367-53-3Relevant academic research and scientific papers
Catalytic, transition-metal-free semireduction of propiolamide derivatives: Scope and mechanistic investigation
Grams, R. Justin,Garcia, Christopher J.,Szwetkowski, Connor,Santos, Webster L.
, p. 7013 - 7018 (2020/09/12)
We report a transition-metal-free trans-selective semireduction of alkynes with pinacolborane and catalytic potassium tert-butoxide. A variety of 3-substituted primary and secondary propiolamides, including an analog of FK866, a potent nicotinamide mononucleotide adenyltransferase (NMNAT) inhibitor, are reduced to the corresponding (E)-3-substituted acrylamide derivatives in up to 99% yield with >99:1 E/Z selectivity. Mechanistic studies suggest that an activated Lewis acid-base complex transfers a hydride to the α-carbon followed by rapid protonation in a trans fashion.
MODULATORS OF CASPASE-6
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Paragraph 000109; 000128-000133, (2016/04/26)
The current application relates to a pharmaceutical composition for the treatment or amelioration of a neurological disease, wherein the composition comprises a therapeutically effective amount of a caspase-6 inhibitor which is an arylpropynamide derivative. The composition can be formulated for oral or topical administration, subcutaneous, intravenous, or intramuscular injection, infusion, inhalation, or intrthecal injection.
Preparation of arylpropynamides and their reaction with malonyl acid derivatives
Petina, Olgaa. A.,Yakovlev, Igorp. P.,Geffken, Detlef
, p. 803 - 809 (2013/04/10)
Synthesis of arylpropynamides and their reactions with different malonic acid derivatives is described. Treatment of arylpropynamides with unsubstituted malonyl chloride furnished N-(3-arylprop-2-ynoyl)-6-chloro-4-hydroxy-2-oxo-2H- pyran-3-carboxamides; m
