2654-31-1Relevant academic research and scientific papers
COMPOSITIONS AND METHODS FOR BLOCKING SODIUM CHANNELS
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Paragraph 00272; 00273; 00274; 00275; 00276, (2018/08/20)
The disclosure provides methods for treating a subject suffering from a disease associated with sodium channel activity. The method comprises administering to the subject a therapeutically effective amount of a compound according to Formula II or Formula III described in the specification, or a pharmaceutically acceptable salt, prodrug, tautomer, stereoisomer, hydrate, or solvate thereof.
Copper-mediated C(sp3)-H azidation with Me3SiN3: Synthesis of imidazoles from ketones and aldehydes
Xie, Zeqiang,Deng, Jiaojiao,Qiu, Zhiping,Li, Juan,Zhu, Qiang
supporting information, p. 6467 - 6470 (2016/05/24)
The efficient construction of 2,4,5-trisubstituted imidazoles, through a copper-mediated three-component reaction involving ketones, aldehydes, and Me3SiN3, has been developed. During the process, 4 C-N bonds were formed sequentially. Experimental results and DFT calculations suggested that azidation of the alpha methylene group of the ketone was the key C-N bond-forming step.
Substituted azole penta-heterocyclic derivatives and solvothermal one-pot synthesis method and application thereof
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Paragraph 0107; 0108; 0109, (2016/11/02)
The invention belongs to the technical field of organic synthesis and particularly discloses a series of substituted azole penta-heterocyclic derivatives and a solvothermal one-pot synthesis method thereof. By the adoption of the solvothermal one-pot synthesis method for preparing the target product, reaction time is short, a solvent is not prone to volatilization in an airtight system, recycling can be realized, production cost is effectively reduced, the advantages of energy conservation and environment friendliness are achieved, operation is easy, yield is high, and the prepared substituted azole penta-heterocyclic derivatives have good anti-microbial biological activity and excellent photophysical properties such as electron conductivity, the fluorescence property and the ultraviolet property, thereby having very high development and application value.
Highly efficient and eco-friendly protocol to functionalized imidazoles via ring-opening of α-nitro epoxides
Guo, Xiao,Shao, Jiaan,Liu, Huan,Chen, Binhui,Chen, Wenteng,Yu, Yongping
, p. 51559 - 51562 (2015/06/25)
A simple and direct synthesis of functionalized imidazoles from α-nitro-epoxides and amidines was developed. This reaction could proceed smoothly in a highly efficient and eco-friendly manner in moderate to excellent yields. A plausible mechanism has also
Nano indium oxide catalyzed tandem cyclization of amidine with nitroolefin
Mitra, Shubhanjan,Bagdi, Avik Kumar,Majee, Adinath,Hajra, Alakananda
supporting information, p. 4982 - 4985 (2013/08/28)
A tandem cyclization of amidine with nitroolefin has been described using nano In2O3 as an efficient catalyst. The reaction is effective for the preparation of 4,5-unsymmetrically substituted 1-H imidazole in moderate to good yields. The catalyst was successfully reused for four consecutive cycles with similar catalytic activities.
A novel bioglycerol-based recyclable carbon catalyst for an efficient one-pot synthesis of highly substituted imidazoles
Ramesh,Murthy, S. Narayana,Karnakar,Nageswar,Vijayalakhshmi, Kukuma,Prabhavathi Devi, Bethala L.A.,Prasad
supporting information; experimental part, p. 1126 - 1129 (2012/03/26)
The new bioglycerol-based carbon catalyst acts as an efficient, readily available, and reusable catalyst for the synthesis of 2,4,5-trisubstituted imidazoles/1,2,4,5-tetrasubstituted imidazoles, when aromatic aldehyde, ammonium acetate/amine, and 1,2-diketone are reacted in acetonitrile.
DABCO as a mild and efficient catalytic system for the synthesis of highly substituted imidazoles via multi-component condensation strategy
Murthy, S. Narayana,Madhav,Nageswar
scheme or table, p. 5252 - 5257 (2010/11/03)
A simple and efficient protocol for the synthesis of highly substituted imidazoles is developed through the condensation of 1,2-dicarbonyl compound, aldehyde, and ammonium acetate or amine via multi-component condensation strategy. The present method gives good to excellent yields of substituted imidazoles.
4H-imidazoles and imidazoles from anionic and dipolar electrocyclization reactions of 2,4-diazapenta-1,3-dienes
Habersaat, Nils,Froehlich, Roland,Wuerthwein, Ernst-Ulrich
, p. 2567 - 2581 (2007/10/03)
1-Amino-2,4-diazapenta-1,3-dienes 5 are synthesized by the activation of N-acylamidines 2 with trifluoromethanesulfonic anhydride and subsequent condensation with amino compounds 4. When the amino compounds 4 possess electron-withdrawing substituents (e.g. alkoxycarbonyl groups, fluorenyl derivatives) this condensation leads instead to 4H-imidazoles 6 and imidazoles 7. These reactions are considered to be 1,5-dipolar electrocyclization reactions of 1,5-dipoles that are tautomers of the 2,4-diazapenta-1,3-dienes 5. Deprotonation of 5b,f by the use of strong organic bases yields the corresponding imidazoles 7b,c after amine elimination during the anionic 1,5-electrocyclization reaction. Results of quantum chemical model calculations (RHF, MP2, SCS-MP2, G3, DFT) performed on the parent 2,4-diazapentadienyl anion 9a, its lithium compound 9a-Li, the corresponding 1,5-dipole 12 and their substituted derivatives are in accordance with the suggested reaction mechanism. X-ray data are given for the 2,4-diazapenta-1,3-dienes 5a·F 3CSO3H, 5c, 5d·F3CSO3H, 5e,f and the spirocyclic 4H-imidazole derivatives 6b-d. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
Hypervalent iodine in synthesis 81: A one-pot procedure for the synthesis of 1H-imidazole derivatives by cyclocondensation of ketones with [Hydroxy(tosyloxy)iodo]benzene and amidines
Zhang,Chen
, p. 2075 - 2077 (2007/10/03)
Tosyloxylation of ketones with [hydroxy(tosyloxy)iodo]benzene (HTIB), followed by treatment with amidines provides a one-pot procedure for the synthesis of 1H-imidazole derivatives with good yields.
