13961-05-2Relevant articles and documents
Synthesis and evaluation of 1H-pyrrole-2,5-dione derivatives as cholesterol absorption inhibitors for suppressing the formation of foam cells and inflammatory response
Yuan, Xinrui,Xia, Yineng,Lu, Peng,Zhu, Lijuan,Zhong, Yuejiao,Wang, Yubin
, p. 1435 - 1447 (2018)
Excess lipid accumulation in the arterial intima and formation of macrophage-derived foam cells in the plaque could cause atherosclerotic lesion. Cholesterol absorption inhibitors could suppress the lipid accumulation of human macrophage, inflammatory res
DMSO-Enabled Selective Radical O?H Activation of 1,3(4)-Diols
Han, Bing,Jiao, Ning,Jin, Rui,Liu, Guoquan,Liu, Jianzhong,Zhang, Ziyao,Zhu, Yuchao
supporting information, p. 19851 - 19856 (2020/09/04)
Control of selectivity is one of the central topics in organic chemistry. Although unprecedented alkoxyl-radical-induced transformations have drawn a lot of attention, compared to selective C?H activation, selective radical O?H activation remains less explored. Herein, we report a novel selective radical O?H activation strategy of diols by combining spatial effects with proton-coupled electron transfer (PCET). It was found that DMSO is an essential reagent that enables the regioselective transformation of diols. Mechanistic studies indicated the existence of the alkoxyl radical and the selective interaction between DMSO and hydroxyl groups. Moreover, the distal C?C cleavage was realized by this selective alkoxyl-radical-initiation protocol.
3,4-diaryl maleimide derivative and preparation method and application thereof
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Paragraph 0091; 0092; 0093, (2017/08/23)
The invention discloses a 3,4-diaryl maleimide derivative represented by a general formula I and a medicinal salt form thereof. The invention further discloses a preparation method of the mentioned 3,4-diaryl maleimide derivative and application of the 3,
Identification of novel small-molecule inhibitors targeting menin-MLL interaction, repurposing the antidiarrheal loperamide
Yue, Liyan,Du, Juanjuan,Ye, Fei,Chen, Zhifeng,Li, Lianchun,Lian, Fulin,Zhang, Bidong,Zhang, Yuanyuan,Jiang, Hualiang,Chen, Kaixian,Li, Yuanchao,Zhou, Bing,Zhang, Naixia,Yang, Yaxi,Luo, Cheng
supporting information, p. 8503 - 8519 (2016/09/28)
Leukemia with a mixed lineage leukemia (MLL) rearrangement, which harbors a variety of MLL fusion proteins, has a poor prognosis despite the latest improved treatment options. Menin has been reported to be a required cofactor for the leukemogenic activity of MLL fusion proteins. Thus, the disruption of the protein-protein interactions between menin and MLL represents a very promising strategy for curing MLL leukemia. Making use of menin-MLL inhibitors with a shape-based scaffold hopping approach, we have discovered that the antidiarrheal loperamide displays previously unreported mild inhibition for the menin-MLL interaction (IC50 = 69 ± 3 μM). In an effort to repurpose this drug, a series of chemical modification analyses was performed, and three of the loperamide-based analogues, DC-YM21, DC-YM25 and DC-YM26 displayed better activities with IC50 values of 0.83 ± 0.13 μM, 0.69 ± 0.07 μM and 0.66 ± 0.05 μM, respectively. Further treatment with DC-YM21 demonstrated potent and selective blockage of proliferation and induction of both cell cycle arrest and differentiation of leukemia cells harboring MLL translocations, which confirmed the specific mechanism of action. In conclusion, molecules of a novel scaffold targeting menin-MLL interactions were reported and they may serve as new potential therapeutic agents for MLL leukemia.
Synthesis of oxazolidin-2-ones and imidazolidin-2-ones directly from 1,3-diols or 3-amino alcohols using iodobenzene dichloride and sodium azide
He, Tian,Gao, Wen-Chao,Wang, Wei-Kun,Zhang, Chi
supporting information, p. 1113 - 1118 (2014/04/03)
A general and efficient method for the synthesis of oxazolidin-2-ones and imidazolidin-2-ones directly from 1,3-diols and 3-amino alcohols has been developed using the same reagent combination of iodobenzene dichloride (PhICl2) and sodium azide (NaN3).
A new approach to the synthesis of 1-oxaspiro[4.n]alkanes and tetrahydrofurans by the 1,5-CH insertion reaction of magnesium carbenoids
Satoh, Tsuyoshi,Yasoshima, Tsukasa,Momochi, Hitoshi
scheme or table, p. 2074 - 2077 (2012/07/14)
1-Alkoxy-1-[2-chloro-2-(p-tolylsulfinyl)ethyl]cycloalkanes were prepared from various cyclic ketones in good overall yields. Treatment of these cycloalkanes bearing a sulfinyl group with i-PrMgCl resulted in the formation of 1-oxaspiro[4.n]alkanes in high to quantitative yields via the 1,5-CH insertion reaction of generated magnesium carbenoid intermediates. When this procedure was commenced with acyclic ketones, multi-substituted tetrahydrofurans were obtained in up to a 96% yield. This procedure provides a new and good way for the synthesis of 1-oxaspiro[4.n]alkanes and tetrahydrofurans with the formation of a carbon-carbon bond between a carbenoid carbon and a non-activated carbon in high yields. The oxygen atom in the magnesium carbenoid intermediates was proved to act very important roles in the 1,5-CH insertion reaction.
Base-catalyzed dehydrogenative Si-o coupling of dihydrosilanes: Silylene protection of diols
Grajewska, Agnieszka,Oestreich, Martin
supporting information; experimental part, p. 2482 - 2484 (2010/11/18)
The direct dehydrogenative coupling of 1,3- and 1,4-diols and dihydrosilanes is efficiently catalyzed by CsO(10 mol%), cleanly affording six- and seven-membered 1,3-dioxo-2-silacycles with dihydrogen as the sole by-product. Conversely, 1,2-diols do not yield the expected 1,3-dioxo-2- silacyclopentanes, essentially forming cyclic disiloxanes instead. Aside from the synthetic convenience, the procedure itself is also useful for straight-forward diol derivatization prior to GLC analysis. Georg Thieme Verlag Stuttgart · New York.
Generation of γ-oxy-substituted benzylithium derivatives by reductive lithiation of 4-phenyl-1,3-dioxanes
Azzena, Ugo,Pilo, Luciano
, p. 664 - 668 (2007/10/03)
Reductive cleavage of 1,3-dioxanes 1a-c with Li metal in the presence of a catalytic amount of naphthalene in THF, followed by reaction with different electrophiles, allowed the synthesis of 3-substituted- and 3,3-disubstituted- 3-phenylpropan-1-ols 4 in good yields.
Effect of Restricted Mobility of the Linking Chain on Intramolecular Excimer Formation
Todesco, R.,Bockstaele, D. Van,Gelan, J.,Martens, H.,Put, J.,Schryver, F. C. De
, p. 4963 - 4968 (2007/10/02)
Intramolecular excimer formation in a series of phenyl-substituted 1,3-propanediols, compounds in which the motions of the linking chain are restricted by intramolecular hydrogen bonding, was investigated under stationary conditions in n-hexane.The excime
The Oxidation of 3,3-Diphenyl-2-propenoic Acid with Manganese(III) Acetate
Kurosawa, Kazu,Tsujita, Tsuyoshi
, p. 2391 - 2394 (2007/10/02)
The oxidation of 3,3-diphenyl-2-propenoic acid with manganese(III) acetate in boiling acetic gave 3,3-diphenyl-2-propenyl acetate, 4-acetoxymethyl-5,5-diphenyltetrahydro-2-furanone, 3,3-diphenyl-2-propenal, 5,5-diphenyl-2,5-dihydro-2-furanone, 4-acetoxy-5,5-diphenyltetrahydro-2-furanone, benzophenone, and 2-oxo-5,5-diphenyltetrahydro-4-furancarboxylic acid.The reaction pathways are discussed.
