- Nickel-Catalyzed Direct Synthesis of Quinoxalines from 2-Nitroanilines and Vicinal Diols: Identifying Nature of the Active Catalyst
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The inexpensive and simple NiBr2/1,10-phenanthroline system-catalyzed synthesis of a series of quinoxalines from both 2-nitroanilines and 1,2-diamines is demonstrated. The reusability test for this system was performed up to the seventh cycle, which afforded good yields of the desired product without losing its reactivity significantly. Notably, during the catalytic reaction, the formation of the heterogeneous Ni-particle was observed, which was characterized by PXRD, XPS, and TEM techniques.
- Shee, Sujan,Panja, Dibyajyoti,Kundu, Sabuj
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p. 2775 - 2784
(2020/03/13)
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- Cooperative iridium complex-catalyzed synthesis of quinoxalines, benzimidazoles and quinazolines in water
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Herein, an efficient methodology for the synthesis of a diverse class of N-heterocyclic moieties, such as quinoxalines, benzimidazoles and quinazolines, was developed in water using bio-renewable alcohols. The quinoxalines were successfully synthesized from a wide range of diamines and nitroamines with diols in air. Interestingly, benzimidazoles and quinazolines were synthesized with excellent isolated yields without using any external base. Finally, the preparative scale synthesis of various N-heterocycles and pharmaceutically active quinoxalines established the practicability of this protocol. For this iridium system, a metal-ligand cooperative mechanism was proposed based on kinetic and DFT studies.
- Chakrabarti, Kaushik,Maji, Milan,Kundu, Sabuj
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supporting information
p. 1999 - 2004
(2019/04/27)
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- Platelet-derived growth factor receptor inhibitor AG1296 preparation method (by machine translation)
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The invention discloses a platelet-derived growth factor receptor inhibitor AG1296 preparation method, in order to 3 - (3, 4 - dimethyl practiced amino) - 3 - phenyl - acrylate as raw materials synthesis. The invention can greatly reduce the AG1296 synthesis cost, has wide application. (by machine translation)
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- Accessing Quinoxalines by Ring-Opening/Cyclization/Detosylation/Aromatization of Activated Aziridines with 2-Bromoanilines: Synthesis of Tyrphostin AG 1296
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Substituted 2-arylquinoxalines have been synthesized by an unprecedented CuI-catalyzed ring-opening/cyclization reaction followed by detosylation/aromatization of activated aziridines with 2-bromoanilines. The transformation efficiently accommo
- Kumar Shahi, Chandan,Pradhan, Sajan,Bhattacharyya, Aditya,Kumar, Raushan,Ghorai, Manas K.
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p. 3487 - 3495
(2017/07/04)
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- Copper-catalyzed aerobic oxidative coupling of o-phenylenediamines with 2-aryl/heteroarylethylamines: direct access to construct quinoxalines
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A copper-catalyzed oxidative coupling reaction of o-phenylenediamines with 2-aryl/heteroarylethylamines using molecular oxygen as an oxidant has been developed. This approach provides a practical and direct access to construct quinoxalines in excellent yields at room temperature. The reaction has a broad substrate scope and exhibits excellent functional-group tolerance. This method could be easily scaled up and applied to the synthesis of biologically active molecules bearing a quinoxaline structural scaffold.
- Gopalaiah, Kovuru,Saini, Anupama,Chandrudu, Sankala Naga,Rao, Devarapalli Chenna,Yadav, Harsh,Kumar, Binay
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p. 2259 - 2268
(2017/03/20)
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- Synthesis of 2-arylquinoxalines: Triarylstibane-catalyzed oxidative cyclization of α-hydroxy ketones with 1,2-diamines under aerobic conditions
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The reaction of α-hydroxy ketones with 1,2-diamines in the presence of triphenylstibane (10 mol%) as catalyst led to the formation of 2-arylquinoxalines in moderate to good yield under aerobic conditions. This reaction is the first example of oxidative cy
- Matsumura, Mio,Takada, Rie,Ukai, Yuu,Yamada, Mizuki,Murata, Yuki,Kakusawa, Naoki,Yasuike, Shuji
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- Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
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This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.
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- Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: Structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins
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A series of 3-indoleacrylonitrile tyrphostins, 2-chloro-3- phenylquinolines, and 3-arylquinoxalines were prepared and tested for inhibition of platelet-derived growth factor receptor tyrosine kinase (PDGF- RTK) activity. The potency of the inhibitors was found to be quinoxalines > quinolines > indoles. Lipophilic groups (methyl, methoxy) in the 6 and 7 positions and phenyl at the 3 position of quinoxalines and quinolines were essential for potency, in contrast to the hydrophilic catechol group in tyrphostins active against EGFR kinase inhibition at different sites. The inhibitors showed selectivity for PDGF and were not active against EGF receptor and HER-2/c-ErbB-2 receptor.
- Gazit, Aviv,App, Harald,McMahon, Gerald,Chen, Jefferey,Levitzki, Alexander,Bohmer, Frank D.
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p. 2170 - 2177
(2007/10/03)
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