939-80-0Relevant articles and documents
Method for synthesizing 4 - chlorine -3 - nitrotoluene carbonitrile by using microchannel reactor (by machine translation)
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Paragraph 0023-0066, (2020/12/09)
4 -chlorobenzonitrile is dissolved in an organic solvent -3 - to obtain 4 -chlorobenzonitrile solution, and 1 chlorobenzonitrile solution and nitric acid and sulfuric acid mixed acid are respectively introduced into the microchannel reactor to react and then enter into the enhanced mass transfer module and the direct flow micro-channel module to obtain solid and dry matter after being washed to obtain 4 - 4 - chlorine -3 - 4 - nitrobenzonitrile. The method has the advantages of simple operation, mild reaction conditions, rapid reaction, high yield, continuous production and the like, solves the safety problem of nitration reaction, and is high in practicability; and the synthesized 4 - chlorine -3 - nitrotoluene carbonitrile is particularly suitable as an intermediate for preparing asatinib hydrochloride. (by machine translation)
Palladium-Catalyzed Cyanation of Aryl Halides Using Formamide and Cyanuric Chloride as a New “CN” Source
Niknam, Esmaeil,Panahi, Farhad,Khalafi-Nezhad, Ali
, p. 2699 - 2707 (2020/04/08)
A new source of “CN” employing formamide and cyanuric chloride is introduced for the cyanation reactions. The treatment of formamide and 2,4,6-trichloro-1,3,5-triazine (TCT; cyanuric chloride) afforded an efficient cyanating agent which it can be used as a nontoxic, readily available, and non-expensive reagent in the cyanation transformations. In this study, palladium-catalyzed cyanation of aryl halides was successfully accomplished using this new “CN” source in high yields.
Development of highly active anti-: Pneumocystis bisbenzamidines: Insight into the influence of selected substituents on the in vitro activity
Maciejewska,Zabiński,Rezler,Ka?mierczak,Collins,Ficker,Cushion
supporting information, p. 2003 - 2011 (2017/10/27)
Here we describe the potency of 21 pentamidine analogues against the fungal pathogen, Pneumocystis carinii, in an ATP bioluminescent assay with toxicity profiles in 2 mammalian cell lines. Reduction of two 5-methyl-1,2,4-oxadiazole rings was applied to the synthesis of acid-labile bisamidines. Anti-Pneumocystis activity is discussed in the context of 3 groups of compounds depending on the main structural changes of the pentamidine lead structure. The groups include: 1) 1,4-bis(methylene)piperazine derivatives 1-5; 2) alkanediamide derivatives 6-10; 3) alkane-derived bisbenzamidines 11-21. IC50 values of 18 compounds were lower than the IC50 of pentamidine. Four bisamidines were active at nanogram concentrations. Introduction of sulfur atoms in the alkane bridge, replacement of the amidino groups with imidazoline rings, or attachment of nitro or amino groups to the benzene rings is responsible for remarkable activity of the new leading structures. The vast majority of compounds, including four highly active ones, can be classified as mild or nontoxic to host cells. These compounds show promise as candidates for new anti-Pneumocystis agents.