- SMALL MOLECULE ACTIVATORS OF NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NAMPT) AND USES THEREOF
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Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.
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Paragraph 00950
(2018/08/03)
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- Aryl alkyl, aryl aryl thioether compound and its synthesis method
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The invention discloses a synthesis method of an aryl-alkyl and aryl-aryl thioether compound represented by a formula (III). According to the synthesis method, aryl tetrafluoroboric acid diazonium salt is taken as a reaction raw material in a reaction solvent, aryl and alkyl thiosulfate is taken as a sulfurizing agent, and the materials react under the catalysis action of visible light and a photosensitive agent to obtain the aryl-alkyl and aryl-aryl thioether compound. According to the synthesis method, the raw materials are easy to obtain and are cheap, the reaction operation is simple, the reaction condition is mild and environment-friendly, the yield is higher, the functional group tolerance is excellent, later modification of drugs is successfully realized, and an efficient C-S bond construction method is provided for medicinal chemistry and biological orthogonal chemistry research.
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Paragraph 0119-0122
(2017/08/16)
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- An aryl alkyl thioether compound and its synthetic method
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The invention discloses a synthetic method of an aryl alkyl thioether compound shown as formula (II), and the synthetic method is as follows: at room temperature and in a water phase, using triazene and haloalkane as reaction raw materials, using Na2S2O3 as a vulcanization reagent for reaction under the promotion effect of a copper catalyst and a Lewis acid to obtain the aryl alkyl thioether compound. The advantages of the synthetic method are as follows: reaction is efficient and yield is high; the vulcanization reagent is cheap, easy to obtain, stable, and free of irritating smell; the reaction is carried out in the solvent green water, the reaction is free of addition of a phase transfer catalyst and a volatile organic solvent, and is environmentally friendly; the reaction is carried out at room temperature, is mild in condition; the catalyst copper sulfate used in the reaction is cheap and economic reaction; the reaction substrate is easy in preparation; after amplification, the reaction efficiency is higher.
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Paragraph 0126-0129
(2019/02/04)
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- Mechanistic Study of a Photocatalyzed C-S Bond Formation Involving Alkyl/Aryl Thiosulfate
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This study presents thioether construction involving alkyl/aryl thiosulfates and diazonium salt catalyzed by visible-light-excited [Ru(bpy)3Cl2] at room temperature in 44-86 % yield. Electron paramagnetic resonance studies found that thiosulfate radical formation was promoted by K2CO3. Conversely, radicals generated from BnSH or BnSSBn (Bn=benzyl) were clearly suppressed, demonstrating the special property of thiosulfate in this system. Transient absorption spectra confirmed the electron-transfer process between [Ru(bpy)3Cl2] and 4-MeO-phenyl diazonium salt, which occurred with a rate constant of 1.69×109 M-1 s-1. The corresponding radical trapping product was confirmed by X-ray diffraction. The full reaction mechanism was determined together with emission quenching data. Furthermore, this system efficiently avoided the over-oxidation of sulfide caused by H2O in the photoexcited system containing Ru2+. Both aryl and heteroaryl diazonium salts with various electronic properties were investigated for synthetic compatibility. Both alkyl- and aryl-substituted thiosulfates could be used as substrates. Notably, pharmaceutical derivatives afforded late-stage sulfuration smoothly under mild conditions.
- Li, Yiming,Xie, Weisi,Jiang, Xuefeng
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supporting information
p. 16059 - 16065
(2015/11/03)
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- Sulfide synthesis through copper-catalyzed C-S bond formation under biomolecule-compatible conditions
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We report here an efficient and mild method for constructing C-S bonds. The reactions were carried out with Na2S2O3 as a sulfurating reagent, CuSO4 as a catalyst, and water as solvent without any surfactant. The products were achieved in moderate to excellent yields at room temperature under air. Notably, this reaction is compatible with various biomolecules including amino acids, oligosaccharides, nucleosides, proteins, and cell lysates. This journal is
- Zhang, Yonghong,Li, Yiming,Zhang, Xiaomei,Jiang, Xuefeng
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supporting information
p. 941 - 944
(2015/01/09)
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- A highly efficient Cu-catalyzed S-transfer reaction: From amine to sulfide
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A highly efficient Cu-catalyzed dual C-S bonds formation reaction, proceeding in alcohol and water under air, is reported, in which inodorous stable Na2S2O3 is used as a sulfurating reagent. This powerful strategy provides a practical and efficient approach to construct thioethers, using readily available aromatic amines and alkyl halides as starting materials. Sensitive and synthetic useful functional groups could be tolerated. Furthermore, pharmaceuticals, glucose, an amino acid, and a chiral ligand are successfully furnished by this late-stage sulfuration strategy.
- Li, Yiming,Pu, Jiahua,Jiang, Xuefeng
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supporting information
p. 2692 - 2695
(2014/06/09)
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