4623-24-9Relevant articles and documents
Assembly of α-(Hetero)aryl Nitriles via Copper-Catalyzed Coupling Reactions with (Hetero)aryl Chlorides and Bromides
Chen, Ying,Xu, Lanting,Jiang, Yongwen,Ma, Dawei
supporting information, p. 7082 - 7086 (2021/02/26)
α-(Hetero)aryl nitriles are important structural motifs for pharmaceutical design. The known methods for direct synthesis of these compounds via coupling with (hetero)aryl halides suffer from narrow reaction scope. Herein, we report that the combination of copper salts and oxalic diamides enables the coupling of a variety of (hetero)aryl halides (Cl, Br) and ethyl cyanoacetate under mild conditions, affording α-(hetero)arylacetonitriles via one-pot decarboxylation. Additionally, the CuBr/oxalic diamide catalyzed coupling of (hetero)aryl bromides with α-alkyl-substituted ethyl cyanoacetates proceeds smoothly at 60 °C, leading to the formation of α-alkyl (hetero)arylacetonitriles after decarboxylation. The method features a general substrate scope and is compatible with various functionalities and heteroaryls.
Preparation method for arylamine compounds
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Paragraph 0049-0050, (2017/09/26)
The invention relates to a preparation method for arylamine compounds, belonging to the fields of medical and chemical intermediate and related chemical technologies. The preparation method comprises the following steps: (1) adding nitro-substituted aromatic compounds, a nanometer porous metal catalyst and a solvent into a reaction vessel, introducing hydrogen and carrying out heating and stirring; and (2) after completion of reaction, subjecting a reaction solution obtained in the step (1) to pressure reduction so as to remove the solvent and carrying out column chromatography so as to obtain target products, i.e., the arylamine compounds. Compared with the prior art, the invention has the following advantages: the nanometer porous palladium catalyst used in the method can perform its unique catalytic activity under mild conditions, is convenient to recycle as a catalyst and can be repeatedly used after simple filtering and cleaning; and the catalyst has stable structure and high catalytic activity and is not obviously reduced in catalytic activity after repeated usage, so industrialization of the arylamine compounds is made possible.
Hydrophilic, Potent, and Selective 7-Substituted 2-Aminoquinolines as Improved Human Neuronal Nitric Oxide Synthase Inhibitors
Pensa, Anthony V.,Cinelli, Maris A.,Li, Huiying,Chreifi, Georges,Mukherjee, Paramita,Roman, Linda J.,Martásek, Pavel,Poulos, Thomas L.,Silverman, Richard B.
, p. 7146 - 7165 (2017/09/07)
Neuronal nitric oxide synthase (nNOS) is a target for development of antineurodegenerative agents. Most nNOS inhibitors mimic l-arginine and have poor bioavailability. 2-Aminoquinolines showed promise as bioavailable nNOS inhibitors but suffered from low