939-80-0Relevant articles and documents
Palladium-Catalyzed Cyanation under Mild Conditions: A Case Study to Discover Appropriate Substrates among Halides and Pseudohalides
Rajendra, Merla Arjuna,Sunil,Sajith, Ayyiliath Meleveetil,Joy, Muthipeedika Nibin,Bakulev, Vasiliy A.,Haridas, Karickal Raman
supporting information, p. 1629 - 1633 (2020/09/15)
A case study has been effectively carried out to identify a suitable substrate among halides and pseudohalides for the palladium-catalyzed cyanation reactions under mild conditions. Among the various substrates considered for evaluation, aryl pentafluorobenzenesulfonates and nonaflates were identified to be the best substrates when compared to corresponding halides and pseudohalides. The substoichiometric use of nontoxic, environmentally benign potassium hexacyanoferrate as a cyanide source and exceptionally milder conditions further highlights the significance of the protocol developed. A wide range of electronically biased and sterically challenging substrates provided the corresponding the nitriles in good to excellent yields.
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)
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
, 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.