1671-82-5Relevant academic research and scientific papers
COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
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Page/Page column 160, (2020/08/22)
The invention relates to a compound of Formula I, pharmaceutical compositions comprising a compound of Formula I, and pharmaceutically acceptable slats thereof, pharmaceutical compositions comprising such compounds and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I to a subject in need thereof.
Alkylation method for nitrogen-hydrogen containing compounds and application thereof
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Paragraph 0051-0053; 0059; 0060, (2018/10/04)
The invention discloses an alkylation method for nitrogen-hydrogen containing compounds and an application thereof, belonging to the technical field of synthesis of organic compounds. The invention provides a series of methods for a nitrogen alkylation reaction of N-H containing heterocyclic compounds (II) with N,N-dimethylformamide dialkyl acetal as an alkyl source under the condition of no participation of metals, and a product with a hydrogen atom on a nitrogen atom substituted by R1 is obtained. The method provided by the invention has the advantages of highly-efficient reaction, high yield, simple treatment after the reaction, simple and convenient operation, mild reaction conditions, no participation of the metals, high tolerance of functional groups of a reaction substrate, wide range and easy preparation of the substrate, high reaction efficiency after amplification of the reaction, and applicability to large-scale industrial production.
INHIBITORS OF BRUTON'S TYROSINE KINASE
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Paragraph 00798, (2016/01/25)
Disclosed herein are compounds that inhibit Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
Molten-state nitration of substituted imidazoles: New synthetic approaches to the novel melt-cast energetic material, 1-methyl-2,4,5-trinitroimidazole
Duddu, Raja,Zhang, Mao-Xi,Damavarapu, Reddy,Gelber, Nathaniel
experimental part, p. 2859 - 2864 (2011/10/18)
Novel, one-step synthetic routes for the preparation of 1-methyl-2,4,5-trinitroimidazole (MTNI) are described. In addition, a new, molten-state nitration method for the synthesis of 1-methyl-2,4,5- trinitroimidazole is developed. Georg Thieme Verlag Stuttgart - New York.
Melt-cast explosive material
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Page/Page column 7, (2008/06/13)
1-Methyl-2,4,5-Trinitroimidazole is synthesized starting from 4-nitroimidazole using stepwise nitration method and further methylation using Dimethylsulphate. It is relatively insensitive to impact and its thermal stability is excellent. The calculated detonation properties indicate that its performance is about 30% better than TATB. It can be prepared easily, with reasonable yield, starting from commercially available Imidazole. Results from impact sensitivity, friction sensitivity, time-to-explosion temperature and vacuum stability tests indicate that it is less sensitive than both RDX and HMX. The good oxygen balance and measured heat of formation data of this material indicate that its propellant performance should be good.
Strategies toward the design of energetic ionic liquids: Nitro- and nitrile-substituted N,N′-dialkylimidazolium salts
Katritzky, Alan R.,Yang, Hongfang,Zhang, Dazhi,Kirichenko, Kostyantyn,Smiglak, Marcin,Holbrey, John D.,Reichert, W. Matthew,Rogers, Robin D.
, p. 349 - 358 (2007/10/03)
Twelve novel 1,3-dialkylimidazolium salts containing strongly electron-withdrawing nitro- and cyano-functionalities directly appended to the cationic heterocyclic rings have been synthesized; the influences of the substituents on both formation and thermal properties of the resultant ionic liquids have been determined by DSC, TGA, and single crystal X-ray diffraction, showing that an electron-withdrawing nitro-substituent can be successfully appended and has a similar influence on the melting behaviour as that of corresponding methyl group substitution. Synthesis of di-, or trinitro-substituted 1,3-dialkylimidazolium cations was unsuccessful due to the resistance of dinitro-substituted imidazoles to undergo either N-alkylation or protonation, while 1-alkyl-4,5-dicyanoimidazoles were successfully alkylated to obtain 1,3-dialkyl-4,5-dicyanoimidazolium salts. Five crystal structures (one of each cation type) show that, in the solid state, the NO2-group has little significant effect, beyond the steric contribution, on the crystal packing. the Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2006.
