- Electro-oxidative C-H alkylation of quinoxalin-2(1: H)-ones with organoboron compounds
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Radical cleavage of C-B bonds to accomplish C-H functionalization is synthetically appealing but practically challenging. We report herein a mild electro-oxidative method for efficient C-H alkylation of quinoxalin-2(1H)-ones by means of radical addition reactions of alkyl boronic acids and esters and alkyl trifluoroborates to afford C-C coupled products. This journal is
- Niu, Kaikai,Hao, Yanke,Song, Lingyun,Liu, Yuxiu,Wang, Qingmin
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supporting information
p. 302 - 306
(2021/01/28)
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- Electro-oxidative C-H azolation of quinoxalin-2(1H)-ones
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We have developed a practical, general protocol for direct C-H azolation reactions of quinoxalin-2(1H)-ones by electro-oxidative cross-coupling. These mild reactions proceed under metal-, oxidant-, and reagent-free conditions to provide synthetically useful azolated quinoxalin-2(1H)-ones. Furthermore, the reactions can be carried out with a pencil lead as an electrode and a 3 V battery as a power source, revealing the remarkable flexibility of this protocol.
- Ding, Ling,Hao, Yanke,Liu, Yuxiu,Niu, Kaikai,Song, Hongjian,Wang, Qingmin,Zhou, Pan
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supporting information
p. 3246 - 3249
(2021/05/21)
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- Rapid alkenylation of quinoxalin-2(1H)-ones enabled by the sequential Mannich-type reaction and solar photocatalysis
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Herein, a rapid alkenylation of quinoxalin-2(1H)-ones enabled by a combination of Mannich-type reaction and solar photocatalysis is demonstrated. A wide range of functional groups are compatible, affording the corresponding products in moderate-to-good yields. Control experiments illustrate that the in situ generated 1O2 plays a central role in this reaction. This green and efficient strategy provides a practical solution for the synthesis of potentially bioactive compounds that containing a 3,4-dihydroquinoxalin-2(1H)-one structure.
- Huang, Lin,Xu, Jun,He, Lei,Liang, Chenfeng,Ouyang, Yani,Yu, Yongping,Li, Wanmei,Zhang, Pengfei
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supporting information
p. 3627 - 3631
(2021/05/03)
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- Electrochemical decarboxylative C3 alkylation of quinoxalin-2(1: H)-ones with N -hydroxyphthalimide esters
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We have developed a protocol for electrochemical decarboxylative C3 alkylation of a wide range of quinoxalin-2(1H)-ones under metal- and additive-free conditions. N-Hydroxyphthalimide esters derived from chain, cyclic, primary, secondary, and tertiary carboxylic acids with a broad scope proved to be suitable substrates. This operationally simple protocol performed in an undivided cell under constant-current conditions is suitable for late-stage functionalization of quinoxalin-2(1H)-ones. The reactions can even be carried out with a 3 V battery as a power source, which demonstrates that organic electrosynthesis can be accomplished without the need for specialized equipment.
- Niu, Kaikai,Song, Lingyun,Hao, Yanke,Liu, Yuxiu,Wang, Qingmin
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supporting information
p. 11673 - 11676
(2020/10/20)
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- Construction of C(sp2)?C(sp3) Bond between Quinoxalin-2(1H)-ones and N-Hydroxyphthalimide Esters via Photocatalytic Decarboxylative Coupling
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A novel visible-light-driven decarboxylative coupling of alkyl N-hydroxyphthalimide esters (NHP esters) with quinoxalin-2(1H)-ones has been developed. This C(sp2)?C(sp3) bond-forming transformation exhibits excellent substrate generality with respect to both the coupling partners. Of note, a series of 3-primary alkyl-substituted quinoxalin-2(1H)-ones that were difficult to synthesize by previous methods could be obtained in moderate to excellent yields. Additionally, the mild conditions, easy availability of substrates, wide functional group tolerance and operational simplicity make this protocol practical in the synthesis of 3-alkylated quinoxalin-2(1H)-ones.
- Yan, Zhiyang,Sun, Bin,Zhang, Xun,Zhuang, Xiaohui,Yang, Jin,Su, Weike,Jin, Can
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p. 3344 - 3349
(2019/09/06)
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- Hepatitis C virus inhibitors
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Hepatitis C virus inhibitors having the general formula (I) are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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Page/Page column 613
(2017/01/23)
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- Α 7 as intranuclear hydroxynicotinic acetylcholine receptor quinuclidines compd.
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PROBLEM TO BE SOLVED: To provide ligands for the nicotinic α-7 receptor used for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.SOLUTION: The disclosure provides compounds of the specified formula I, including their salts, and compositions and methods using the compounds.
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Paragraph 0296; 0297
(2018/10/03)
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- BIARYL ACETAMIDE COMPOUNDS AND METHODS OF USE THEREOF
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Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
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Paragraph 000178
(2015/03/16)
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- QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS
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The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
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Page/Page column 89
(2009/10/31)
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- NIACIN RECEPTOR AGONISTS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT
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Compounds of the formula (I): as well as pharmaceutically acceptable salts and solvates are disclosed. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and triglycerides, and raising HDL levels. Pharmaceutic
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Page/Page column 35
(2008/06/13)
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- COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS
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The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans.
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Page/Page column 133-134
(2010/11/25)
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- Synthesis and SAR of novel imidazoquinoxaline-based Lck inhibitors: Improvement of cell potency
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A series of anilino(imidazoquinoxaline) analogues bearing solubilizing side chains at the 6- and 7-positions of the fused phenyl ring has been prepared and evaluated for inhibition against Lck enzyme and of T-cell proliferation. Significant improvement of the cellular activity was achieved over the initial lead, compound 2.
- Chen, Ping,Iwanowicz, Edwin J.,Norris, Derek,Gu, Henry H.,Lin, James,Moquin, Robert V.,Das, Jagabandhu,Wityak, John,Spergel, Steven H.,De Fex, Henry,Pang, Suhong,Pitt, Sydney,Shen, Ding Ren,Schieven, Gary L.,Barrish, Joel C.
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p. 3153 - 3156
(2007/10/03)
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- Synthesis of thieno[2,3-b]quinoxalines and pyrrolo[1,2-a]-quinoxalines from 2-haloquinoxalines
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The palladium(0)-catalysed coupling of 2-haloquinoxalines with functionally substituted alkynes, addition of one mol equivalent of bromine to the 2-alkynylquinoxalines thus produced and then reaction of the resulting dibromides with disodium trithiocarbon
- Armengol,Joule
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p. 978 - 984
(2007/10/03)
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- Quinoxaline Derivatives. XII. The Reactions of Quinoxaline 1,4-Dioxides with Acetic Anhydride
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Quinoxaline 1,4-dioxide (XIIIa) with acetic anhydride gave 1-acetoxy-2(1H)-quinoxalinone (XIVa) which was prone to facile hydrolysis to yield 1-hydroxy-2(1H)-quinoxalinone (XVa).Both XIVa and XVa were isolated from the reaction mixture.On prolonged heating with acetic anhydride, XIIIa, XIVa and XVa were converted slowly to the same end product, 2,3(1H,4H)-quinoxalinedione (XXa). 6-Ethoxy- (XIIIb), 6-methoxy- (XIIIc), and 6-methylquinoxaline 1,4-dioxide (XIIId) behaved similarly, except that the attack of the reagent took place exclusively on N-oxide para to the electron-donating substituents, and none of the other expected isomeric compounds XVIIb-d were isolated.Whereas 6-chloroqinoxaline 1,4-dioxide (XIIIe) bearing an electron-attracting chloro substituent on the benzene ring gave exclusively the other isomers XVIIe, XVIIIe, and XXe.A mechanism for this novel rearrangement is proposed and discussed.
- Ahmed, Yusuf,Qureshi, M. Ikram,Habib, M. Saleem,Farooqi, M. Amir
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p. 1145 - 1148
(2007/10/02)
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- The facile one pot synthesis of 6-substituted 2(1H)-quinoxalinones
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Facile one pot synthesis of 6-substituted 2(1H)-quinoxalinones and these reaction mechanisms are described.The intramolecular cyclization reaction of 4'-substituted 2'-nitroacetoacetanilides in aqueous basic medium and the reduction of 6-substituted 2(1H)-quinoxalinone-4-oxide wit sodium borohydride or sodium hydrogensulfite were studied in detail
- Sakata, Gozyo,Makino, Kenzi,Morimoto, Katsushi
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p. 143 - 151
(2007/10/02)
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