23346-82-9Relevant academic research and scientific papers
N-bromosuccinimide/dibromodimethylhydantoin in aqueous base: A practical method for the bromination of activated benzoic acids
Auerbach, Joseph,Weissman, Steven A.,Blacklock, Thomas J.,Angeles, Marshall R.,Hoogsteen, Karst
, p. 931 - 934 (1993)
A new bromination method employing NBS or dibromodimethylhydantoin in aqueous base is described for the synthesis of 3-bromo-2,6-dimethoxybenzoic acid (1) and other monobrominated alkoxybenzoic acids.
Synthesis of Axially Chiral 2,2′-Bisphosphobiarenes via a Nickel-Catalyzed Asymmetric Ullmann Coupling: General Access to Privileged Chiral Ligands without Optical Resolution
Zuo, Ziqing,Kim, Raphael S.,Watson, Donald A.
supporting information, p. 1328 - 1333 (2021/02/01)
We report an asymmetric homocoupling of ortho-(iodo)arylphosphine oxides and ortho-(iodo)arylphosphonates resulting in highly enantioenriched axially chiral bisphosphine oxides and bisphosphonates. These products are readily converted to enantioenriched b
Access to Atropisomerically En-riched Biaryls by the Coupling of Aryllithiums with Arynes under Control by Homochiral Oxazolines
Yalcouye, Boubacar,Berthelot-Bréhier, Ana?s,Augros, David,Panossian, Armen,Choppin, Sabine,Chessé, Matthieu,Colobert, Fran?oise,Leroux, Frédéric R.
supporting information, p. 725 - 732 (2017/01/18)
We report the preparation of axially stereoenriched biphenyls by the coupling of in situ generated aryllithiums and arynes using chiral oxazoline auxiliaries. The design of the aryne precursors, the choice of oxazoline and the reaction conditions were key to accessing the desired, highly substituted, atropisomerically enriched biarylic products. In one case, the two atropo-diastereomers could be obtained in isomerically pure form by column chromatographic separation and their absolute configurations established by X-ray crystallography. The stereoselectivity of the reaction seems to be governed by subtle parameters.
Compound and application thereof
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Paragraph 0445, (2016/10/09)
The invention discloses a compound and application thereof. The compound is the compound shown in the formula (I) or a stereoisomer or a pharmaceutical acceptable salt or solvate or a prodrug of the compound shown in the formula (I). The compound can restrain tumor cell proliferation through the effect RRM2, and restrain tumor stem cell regeneration, thereby being effectively used for preparing medicine for preventing or treating proliferative diseases and particularly anti-cancer medicine.
A kind of acridine compounds and use thereof
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Paragraph 0041-0043, (2016/11/21)
The invention provides an acridine compound and an application thereof. The compound has a structure as shown in a general formula I described in the specification, wherein R1 is selected from H or -CO-Ph-(o,m,p) R4; R2 is selected from O or -N-Ph-(o,m,p)
Influence of N,N′-Substituted Piperazines on Cytolysis
Veselkina,Solovtsova,Petrishchev,Galebskaya,Borovitov,Nilov,Solov’eva,Vorob’ev,Len’shina
, p. 743 - 748 (2016/07/06)
The hemolytic activity of N,N′-substituted piperazines and their influence on the hemolytic process initiated by radiation (red LED, 653 nm) in the presence of radachlorin (RADA-FARMA, Russia) photosensitizer and on complement-dependent hemolysis were stu
ENHANCING AUTOPHAGY OR INCREASING LONGEVITY BY ADMINISTRATION OF UROLITHINS OR PRECURSORS THEREOF
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Sheet 35, (2014/01/17)
Disclosed are methods, compounds, and compositions useful for increasing autophagy and promoting longevity. The methods, compounds, and compositions relate to urolithins and urolithin precursors and use thereof. Certain urolithins are represented by Formula I, while certain urolithin precursors are represented by Formula IV. The urolithin may be urolithin A, urolithin B, urolithin C, or urolithin D. The urolithin precursor may be ellagic acid or an ellagitannin. The methods include in vivo, ex vivo, and in vitro uses of the compounds and compositions.
Enantioselective synthesis of α-benzylated lanthionines and related tripeptides for biological incorporation into E. coli peptidoglycan
Denol, Thibaut,Zervosen, Astrid,Lemaire, Christian,Joris, Bernard,Herv, Mireille,Blanot, Didier,Zaragoza, Guillermo,Luxen, Andr
supporting information, p. 9853 - 9863 (2015/01/09)
The synthesis of modified tripeptides (S)-Ala-γ-(R)-Glu-X, where X = (R,S) or (R,R) diastereomers of α-benzyl or α-(4-azidobenzyl)lanthionine, was carried out. The chemical strategy involved the enantioselective alkylation of a 4-MeO-phenyloxazoline. The reductive opening of the alkylated oxazolines, followed by cyclization and oxidation, led to four PMB-protected sulfamidates. Subsequent PMB removal, Boc protection and regioselective opening with cysteine methyl ester led to protected lanthionines. These compounds were further converted in a one pot process to the corresponding protected tripeptides. After ester and Boc deprotection, the four tripeptides were evaluated as potential analogues of the natural tripeptide (S)-Ala-γ-(R)-Glu-meso-A2pm. These compounds were evaluated for introduction, by means of the biosynthetic recycling pathway, into the peptidoglycan of Escherichia coli. A successful in vitro biosynthesis of UDP-MurNAc-tripeptides from the tripeptides containing α-benzyl lanthionine was achieved using purified murein peptide ligase (Mpl). Bioincorporation into E. coli W7 did not occur under different tested conditions probably due to the bulky benzyl group at the Cα carbon of the C-terminal amino acid. This journal is
Two-face, two-turn α-helix mimetics based on a cross-acridine scaffold: Analogues of the bim BH3 domain
Li, Xiangqian,Wang, Ziqian,Feng, Yingang,Song, Ting,Su, Pengchen,Chen, Chengbin,Chai, Gaobo,Yang, Ying,Zhang, Zhichao
, p. 1280 - 1285 (2014/06/24)
The design of a cross-acridine scaffold mimicking the i, i+3, i+5, and i+7 residues distributed over a two-face, two-turn α-helix is described. Docking studies and 2D 1H,15N HSQC NMR spectroscopy provide compelling evidence that compound 3-d accurately reproduces the arrangement of four hotspots in the Bim BH3 peptide to permit binding to the Mcl-1 and Bcl-2 proteins (Ki 0.079 and 0.056 μM, respectively). Furthermore, the hotspot mutation could also be mimicked by individual or multiple deletions of side chains on the scaffold. Building site: A cross-acridine scaffold was designed to project functional groups with spatial and angular geometries that accurately mimic the i, i+3, i+5, and i+7 side chains on a two-turn, two-face section of an α-helix. The binding mode of the most potent compound, 3-d, to Mcl-1 was confirmed by 1H, 15N HSQC NMR.
Synthesis of polyhydroxylated flavonoids bearing a lipophilic decyl tail as potential therapeutic antioxidants
Caldwell, Stuart T.,McPhail, Donald B.,Duthie, Garry G.,Hartley, Richard C.
scheme or table, p. 23 - 33 (2012/03/07)
Antioxidants have potential for the treatment of stroke and neurodegeneration, and chimeric compounds that combine a flavon-3-ol head group related to myricetin and a lipophilic decyl tail are known to protect membranes from oxidative damage at least as well as vitamin E. New flavon-3-ols that are highly hydroxylated in the B ring in ways not found in natural flavon-3-ols and bearing a lipophilic decyl tail have been prepared from trimethoxy-and tetramethoxybenzoic acids accessed by lithiation-carboxylation reactions. Direct enolate acylation was preferred over Baker-Venkataraman rearrangement when there were methoxy groups at both the 2-and the 6-position of the benzoic acid derivatives.
