- Sulfonamide compound as sodium channel blocker and application thereof
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The invention provides a sulfonamide compound as a sodium channel blocker and an application of the sulfonamide compound, and the sulfonamide compound has dual inhibitory activity on Nav1.7 and Nav1.3 at the same time and can be used as a medicine for tre
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Paragraph 0057-0061; 0150-0154
(2021/05/08)
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- INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR KINASES
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Provided herein are heteroaryl inhibitors of fibroblast growth factor receptor kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
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Paragraph 001457-001459
(2021/12/28)
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- Tert-amino effect-promoted rearrangement of aryl isothiocyanate: A versatile approach to benzimidazothiazepines and benzimidazothioethers
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A general and practical approach to benzimidazothiazepine and benzimidazothioether derivatives via an intramolecular nucleophilic addition/ring expansion rearrangement of aryl isothiocyanates promoted by the tert-amino effect has been developed. This reaction is catalyzed by low-cost camphorsulfonic acid and tolerates a broad substrate scope with complete atom economy. Structurally intriguing benzimidazothiazepine and benzimidazothioether products could be easily obtained by a simple operation in good to excellent yield (up to 98%).
- Geng, Xinyu,Liu, Siyuan,Qu, Jingping,Wang, Baomin,Wang, Wenyao
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p. 12635 - 12643
(2020/11/09)
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- Cobalt-catalyzed C-N bond-forming reaction between chloronitrobenzenes and secondary amines
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Cyclic secondary amines react with mono- or dichloronitrobenzene in the presence of a catalytic amount of cobalt(II) chloride. Phosphane ligands are beneficial for the reaction, although the bite-angle effect was not strong. The nitro-substituted tertiary amines formed are important as bioactive compounds and can also be intermediates for the synthesis of substituted anilines. This work represents the first cobalt-catalyzed approach to C-N bond-forming reactions involving aromatic chlorides and cyclic secondary amines. The reaction is ortho- and para-selective, with meta-substituted halides being unreactive in this procedure. The first cobalt-catalyzed C-N bond-forming reaction involving aromatic chlorides and cyclic secondary amines is described.The reaction is ortho- and para-selective; meta-substituted halides are unreactive. Copyright
- Toma, Gabriel,Yamaguchi, Ryohei
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experimental part
p. 6404 - 6408
(2011/02/22)
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- 7-PHENYL-ISOQUINOLINE-5-SULFONYLAMINO DERIVATIVES AS INHIBITORS OF AKT (PROTEINKINASE B)
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The present invention relates to compounds Formula (I) as inhibitors of AKT activity, which are useful for the treatment of susceptible neoplasms and viral infections.
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Page/Page column 29
(2010/02/12)
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- Specific features of nucleophilic substitution in 1-chloro-3,4- dinitrobenzene
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Effects of the solvent, temperature, and nucleophile nature on the selectivity of nucleophilic substitution in 1-chloro-3,4-dinitrobenzene were studied, and optimal conditions were found for the synthesis and isolation of particular products.
- Zotova,Kushakova,Kuznetsov,Rodin,Garabadzhiu
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p. 1473 - 1476
(2007/10/03)
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- Reaction of Mono-, Di-, and Trichloronitrobenzenes with N-Methyl Substituted Cyclic Tertiary Amines under High Pressure
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The reactions of mono-, di-, and trichloronitrobenzenes with 1-methylpyrrolidine under high pressure gave products of demethylation and ring-opening through a quaternary pyrrolidinium chloride intermediate formed by the SNAr reaction.On the other hand, the reactions with 1-methylpiperidine and 4-methylmorpholine gave only demethylation products.The selectivities of the resctions of 1-methylpyrrolidine with these chloronitrobenzenes were found to be effected by the neighboring substituent to the pyrrolidinium group.
- Ibata, Toshikazu,Shang, Muhong,Demura, Tetsuo
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p. 2717 - 2726
(2007/10/03)
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- Nucleophilic Substitution Reaction of Aromatic Chlorides with Cyclic Tertiary Amines under High Pressure
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The reaction of p-chloronitrobenzene with N-methylpyrrolidine under high pressure gave demethylation product and ring opening products through quaternary ammonium chloride intermediate formed by the SNAr reaction.On the other hand, the reactions with N-methylpiperidine and N-methylmorpholine gave only demethylation products.The reactions of o-chloronitrobenzene and 2,4-dichloronitrobenzene with above amines gave similar results.
- Ibata, Toshikazu,Shang, Muhong,Demura, Tetsuo
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p. 359 - 362
(2007/10/02)
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- Aromatic Nucleophilic Substitution of Halobenzenes with Amines under High Pressure
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The nucleophilic substitution reactions of aromatic halides having electron-attracting groups on ortho or para position with various primary and secondary amines were accelerated by high pressure to give the corresponding N-substituted anilines in high yields.The bulkiness of amines affects its reactivity to lower the yields of the products.Although the secondary amines are usually less reactive than primary amines, cyclic secondary amines such as morpholine, piperidine, and pyrrolidine were found very reactive. 1,4-Diazabicyclooctane and quinuclidine gave N-quarternary ammonium halides in high yields in contrast to the low reactivity of acyclic tertiary amines.Dichloro- and trichloro-nitrobenzenes also react with diethylamine, pyrrolidine, and morpholine to give mono-, di-, and trisubstitution products depending upon the amount of amine and the position of nitro group in these chlorides.
- Ibata, Toshikazu,Isogami, Yasushi,Toyoda, Jiro
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