- HURAT1 (human urate anion transporter 1) inhibitors and application thereof
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The invention belongs to the field of medicinal chemistry and particularly relates to hURAT1 (human urate anion transporter 1) inhibitors and an application thereof. Specifically, the hURAT1 inhibitors are compounds with structure shown as formula (I) or (II) in the description or pharmaceutically acceptable salts of the compounds. Experiments prove that the compounds have good inhibition effect on uric acid transport of the hURAT1 in an HEK293 transfection cell, which shows that the compounds have good application prospect in treatment of hyperuricemia or gout.
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Paragraph 0064; 0086; 0086; 0088
(2018/11/22)
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- A General One-Pot Synthesis of 2H-Indazoles Using an Organophosphorus–Silane System
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A simple and direct approach for the regioselective construction of the privileged 2H-indazole scaffold is described. The developed one-pot strategy involves phospholene-mediated N?N bond formation to access 2H-indazoles. The amount of organophosphorus reagent was minimized by recycling the phospholene oxide with organosilane reductants. Starting from functionalized 2-nitrobenzaldehydes and primary amines, a mild reductive cyclization, involving the use of commercially available phospholene oxide and silanes, delivered a wide variety of substituted 2H-indazoles in good to excellent yields.
- Schoene, Jens,Bel Abed, Hassen,Schmieder, Peter,Christmann, Mathias,Nazaré, Marc
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supporting information
p. 9090 - 9100
(2018/06/29)
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- A Biphilic Phosphetane Catalyzes N-N Bond-Forming Cadogan Heterocyclization via PIII/PV = O Redox Cycling
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A small-ring phosphacycle, 1,2,2,3,4,4-hexamethylphosphetane, is found to catalyze deoxygenative N-N bond-forming Cadogan heterocyclization of o-nitrobenzaldimines, o-nitroazobenzenes, and related substrates in the presence of hydrosilane terminal reductant. The reaction provides a chemoselective catalytic synthesis of 2H-indazoles, 2H-benzotriazoles, and related fused heterocyclic systems with good functional group compatibility. On the basis of both stoichiometric and catalytic mechanistic experiments, the reaction is proposed to proceed via catalytic PIII/PV = O cycling, where DFT modeling suggests a turnover-limiting (3+1) cheletropic addition between the phosphetane catalyst and nitroarene substrate. Strain/distortion analysis of the (3+1) transition structure highlights the controlling role of frontier orbital effects underpinning the catalytic performance of the phosphetane.
- Nykaza, Trevor V.,Harrison, Tyler S.,Ghosh, Avipsa,Putnik, Rachel A.,Radosevich, Alexander T.
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p. 6839 - 6842
(2017/05/29)
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- Regioselective synthesis of 2 H-indazoles using a mild, one-pot condensation-cadogan reductive cyclization
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An operationally simple and efficient one-pot synthesis of 2H-indazoles from commercially available reagents is reported. Ortho-imino-nitrobenzene substrates, generated via condensation, undergo reductive cyclization promoted by tri-n-butylphosophine to afford substituted 2H-indazoles under mild reaction conditions. A variety of electronically diverse ortho-nitrobenzaldehydes and anilines were examined. To further extend the scope of the transformation, aliphatic amines were also employed to form N2-alkyl indazoles selectively under the optimized reaction conditions.
- Genung, Nathan E.,Wei, Liuqing,Aspnes, Gary E.
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p. 3114 - 3117
(2014/06/23)
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- Palladium Complex-Catalyzed Reductive N-Heterocyclization of Nitroarenes: Novel Synthesis of Indole and 2H-Indazole Derivatives
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The dichlorobis(triphenylphosphine)palladium (PdCl2(PPh3)2)-tin(II)chloride (SnCl2) system shows high catalytic activity for the reductive N-heterocyclization of various 2-nitrostyrene and N-(2-nitrobenzylidene)amine derivatives when employed at 100 deg C for 16 h under 20 kg cm-2 of initial carbon monoxide pressure, to give the corresponding indole and 2H-indazole derivatives in good yield.For example, 2-phenylindole was obtained in 75percent yield from the reductive N-heterocyclization of 2-nitrostilbene.Similarly, 2-propyl-2H-indazole was readily prepared in 83percent yield by the reductive N-heterocyclization of N-(2-nitrobenzylidene)propylamine.A nitrene intermediate for the present reaction is proposed on the basis of deuterium-labeling experiments and the investigation of alkyl rearrangement in the construction of the indole skeleton.Carbon monoxide effectively operates as a deoxygenating agent of the nitro group to afford a nitrene intermediate.
- Akazome, Motohiro,Kondo, Teruyuki,Watanabe, Yoshihisa
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p. 3375 - 3380
(2007/10/02)
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