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All total 31 Articles be found
PROTAC compound for targeted degradation of IDO1, and preparation method and application thereof
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Paragraph 0024-0026; 0036-0037, (2020/06/17)
The invention provides a PROTAC compound represented by formula I and used for targeted degradation of IDO1, and a pharmaceutically acceptable salt, a hydrate or a solvate thereof. In the formula I, Xrepresents -CH2 or -C = O, Y represents -CH2 or -C= O, and n is a natural number from 2 to 9. The PROTAC compound for targeted degradation of the IDO1 has efficient activity of targeted degradation of the IDO1 protein.
Amino-polystyrene supported hexaethylene glycol-bridged ionic liquid as an efficient heterogeneous catalyst for water-mediated nucleophilic hydroxylation
Reddy, Mudumala Veeranarayana,Kang, Seok Min,Yoo, Suah,Woo, Sang Sik,Kim, Dong Wook
, p. 9435 - 9442 (2019/04/01)
We report a simple and eco-friendly method for producing an amino-polystyrene supported hexaethylene glycol-bridged ionic liquid (APS-HEGBIL) based on the copolymerization of amino-styrene with 1-vinyl imidazolium ionic liquid bearing hexaethylene glycol moieties, and its characterization by several analytical techniques. The resulting APS-HEGBIL catalyst was found to be remarkably efficient at catalyzing the selective nucleophilic hydroxylation of alkyl halides to produce the corresponding alcohols in water, which acted as a solvent and a nucleophilic hydroxide source. The catalyst was easily recycled and maintained its catalytic activity and stability after ten cycles with excellent yields. The main attributes of the catalyst were that it significantly enhanced the nucleophilicity of water during reactions and promoted the rapid conversions of polar and base-sensitive alkyl halide reactants to alcohols in excellent yields. The combination of ionic liquids and polymeric materials afforded quasi-homogeneous catalysts that were recycled by simple filtration and provided environmentally benign means for conducted catalytic procedures.
Formation of [2]- and [3]Rotaxanes through Bridging under Kinetic and Thermodynamic Control
Fujino, Takaaki,Naitoh, Hirotake,Miyagawa, Shinobu,Kimura, Masaki,Kawasaki, Tsuneomi,Yoshida, Kazuyuki,Inoue, Hajime,Takagawa, Hiroaki,Tokunaga, Yuji
supporting information, p. 369 - 372 (2018/01/27)
An efficient synthesis of a doubly stranded [3]rotaxane has been developed through bridging of a pseudo[3]rotaxane featuring two axle components. Reversible azine formation was effective as the bridging reaction. Kinetic and thermodynamic conditions provided the [2]- and [3]rotaxanes, respectively.
Preparation method of organic intermediate hexaethylene glycol
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Paragraph 0014; 0015, (2017/06/02)
The invention provides a preparation method of organic intermediate hexaethylene glycol. The preparation method comprises the following steps of: dissolving tetraglycol in tetrahydrofuran, and adding sodium hydride for reaction; after no hydrogen is released, cooling, dropwise adding tert-butyl bromoacetate for reacting overnight; after reaction is finished, adding water, quenching residual sodium hydride, and extracting with ethyl acetate so as to obtain an intermidate compound A; drying the compound A, mixing with silica gel powder, packing column, performing chromatographic purification, dissolving the purified compound A into tetrahydrofuran, cooling, adding lithium aluminium hydride for reacting overnight; after reaction is finished, adding water, quenching residual lithium aluminium hydride, extracting with small polar impurities with dichloromethane, reserving a water phase, adding ion exchange resin until the pH is neutral, filtering out resin, and performing vacuum concentration on the water phase, thereby obtaining organic intermediate hexaethylene glycol. The preparation method is capable of producing a large amount of hexaethylene glycol, not only is convenient to extract and purify and high in final hexaethylene glycol, but also can be applied to series of high polyethylene glycol products with single synthesis.
Nucleophilic Hydroxylation in Water Media Promoted by a Hexa-Ethylene Glycol-Bridged Dicationic Ionic Liquid
Jadhav, Vinod H.,Kim, Jin Gwan,Jeong, Hyeon Jin,Kim, Dong Wook
, p. 7275 - 7280 (2015/07/28)
Hexaethylene glycol bis(3-hexaethylene glycol imidazolium) dimesylate ionic liquid (hexaEG-DHIM) was designed and prepared as a highly efficient promoter for the nucleophilic hydroxylation of alkyl halides to the corresponding alcohol products in neat water media. It was observed that hexaEG-DHIM promoter enhanced the nucleophilicity of water significantly in the reaction. In addition, the hexaEG-DHIM could be reused several times without loss of activity. Moreover, the hydroxylation reactions of base-sensitive and/or polar alkyl halide substrates proceeded highly chemoselectively in excellent yields.