126532-05-6Relevant articles and documents
Strengthening N...X halogen bonding via nitrogen substitution in the aromatic framework of halogen-substituted arylpyrazinamides
Khavasi, Hamid Reza,Hosseini, Mahdieh,Tehrani, Alireza Azhdari,Naderi, Soheila
, p. 4546 - 4553 (2014)
The importance of N...X halogen bonding in a series of N-(5-halo-2-pyridinyl)pyrazine-2-carboxamides has been investigated by different methods. The results show that when nitrogen is substituted for carbon in the aryl backbone of the parent compound, it can affect the electron accepting ability of bromine and iodine substituents. Thus, a stronger halogen bond can be formed. This journal is the Partner Organisations 2014.
Method for selectively synthesizing halogenated arylamine through copper catalysis (by machine translation)
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Paragraph 0087-0090, (2020/12/30)
The method comprises the following steps: reacting a substrate with a halogenating reagent (III) in an organic solvent to obtain a catalyst. The reaction 0 - 80 °C is reacted at 0.5 - 6h under the action of an oxidizing agent, and after the reaction is finished, the reaction liquid is subjected to post-treatment to obtain the product halogenated aromatic amine compound. To the invention, direct synthesis of the halogenated aromatic amine compounds is achieved for the first time, and the problems that in the traditional method, the metal catalyst is expensive, the halogenated reagent toxicity is large, byproducts are large and the like are solved. At the same time, the product can take off the pyridine guide group through simple hydrolysis, and further functional groups can be combined into an aromatic heterocyclic compound. The method is simple and convenient to operate, mild in reaction conditions, high in selectivity, high in product yield and wide in substrate applicability, and is an efficient organic synthesis means. : Substrate: Halogenating agent: Product: (by machine translation)
Synthesis and antitubercular evaluation of N-Arylpyrazine and N,Na-Alkyl-diylpyrazine-2-carboxamide derivatives
Bispo, Marcelle De Lima Ferreira,Goncalves, Raoni Schroeder Borges,Lima, Camilo Henrique Da Silva,Cardoso, Laura Nogueira De Faria,Lourenco, Maria Cristina Silva,De Souza, Marcus Vinicius Nora
, p. 1317 - 1322 (2013/02/22)
Two series of pyrazinamide (PZA) derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Some compounds exhibited minimum inhibitory concentration activity of 50-100 μg/mL, greater than the first line antituberculosis drug PZA in Alamar Blue assay (>100 μg/mL). The obtained activities can be considered promising results, which characterizes these compounds as good start points to development of new antitubercular agents.
