869589-06-0Relevant academic research and scientific papers
Direct transformation of aryl 2-pyridyl esters to secondary benzylic alcohols by nickel relay catalysis
Wu, Xianqing,Li, Xiaobin,Huang, Wenyi,Wang, Yun,Xu, Hui,Cai, Liangzhen,Qu, Jingping,Chen, Yifeng
supporting information, p. 2453 - 2458 (2019/03/29)
A direct transformation of aryl esters to secondary benzylic alcohols via tandem Ni-catalyzed cross-coupling reactions of aromatic 2-pyridyl esters with alkyl zinc reagents and carbonyl group reduction by Ni-H species is achieved. Preliminary mechanistic studies reveal that the Ni-H species is generated in situ via β-hydride elimination of the Negishi reagents. The reaction is catalyzed by bench-stable nickel salts under mild conditions with wide functional group tolerance.
Docking study and biological evaluation of pyrrolidine-based iminosugars as pharmacological chaperones for Gaucher disease
Kato, Atsushi,Nakagome, Izumi,Sato, Kasumi,Yamamoto, Arisa,Adachi, Isao,Nash, Robert J.,Fleet, George W. J.,Natori, Yoshihiro,Watanabe, Yasuka,Imahori, Tatsushi,Yoshimura, Yuichi,Takahata, Hiroki,Hirono, Shuichi
, p. 1039 - 1048 (2016/01/20)
We report on the synthesis and biological evaluation of a series of α-1-C-alkylated 1,4-dideoxy-1,4-imino-d-arabinitol (DAB) derivatives as pharmacological chaperones for Gaucher disease. The parent compound, DAB, did not show inhibition of human β-glucocerebrosidase but showed moderate intestinal α-glucosidase inhibition; in contrast, extension of α-1-C-alkyl chain length gave a series of highly potent and selective inhibitors of the β-glucocerebrosidase. Our design of α-1-C-tridecyl-DAB (5j) produced a potent inhibitor of the β-glucocerebrosidase, with IC50 value of 0.77 μM. A molecular docking study revealed that the α-1-C-tridecyl group has a favorable interaction with the hydrophobic pocket and the sugar analogue part (DAB) interacted with essential hydrogen bonds formed to Asp127, Glu235 and Glu340. Furthermore, α-1-C-tridecyl-DAB (5j) displayed enhancement of activity at an effective concentration 10-times lower than isofagomine. α-1-C-Tridecyl-DAB therefore provides the first example of a pyrrolidine iminosugar as a new class of promising pharmacological chaperones with the potential for treatment of Gaucher disease. 2016 The Royal Society of Chemistry.
Polymer precursor and its manufacturing method for production of nano-ribbon graphene
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Paragraph 0111-0113, (2017/01/02)
An oligophenylene monomer of general formula (I) wherein R1 and R2 are independently of each other H, halogene, —OH, —NH2, —CN, —NO2 or a linear or branched, saturated or unsaturated C1-C40 hydrocarbon residue, which can be substituted 1- to 5-fold with h
POLYMERIC PRECURSORS FOR PRODUCING GRAPHENE NANORIBBONS AND METHODS FOR PREPARING THEM
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Page/Page column, (2014/12/09)
An oligophenylene monomer of general formula (I) wherein R1 and R2 are independently of each other H, halogene, —OH, —NH2, —CN, —NO2 or a linear or branched, saturated or unsaturated C1-C40 /sub
