- Regioselective monobromination of phenols with KBr and ZnAl–BrO3?–layered double hydroxides
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The regioselective mono-bromination of phenols has been successfully developed with KBr and ZnAl–BrO3?–layered double hydroxides (abbreviated as ZnAl–BrO3?–LDHs) as brominating reagents. The para site is much favorable and the ortho site takes the priority if para site is occupied. This reaction featured with excellent regioselectivity, cheap brominating reagents, mild reaction condition, high atom economy, broad substrate scope, and provided an efficient method to synthesize bromophenols.
- Wang, Ligeng,Feng, Chun,Zhang, Yan,Hu, Jun
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- Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design
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GPR120 is an attractive target for the treatment of type 2 diabetes. In this study, a series of biphenyl derivatives were designed, synthesized by hybrid design. The selected compound 6a exhibited potent GPR120 agonist activity (EC50 = 93 nM) and high selectivity over GPR40. The results of oral glucose tolerance test (OGTT) demonstrated that 6a exhibited significant glucose-lowering effect in glucose-loaded ICR male mice. Analysis of the structure–activity relationship is also presented. Compound 6a deserves further biological evaluation and structural modifications.
- Sheng, Ren,Yang, Liu,Zhang, Yanchun,Xing, Enming,Shi, Rui,Wen, Xiaoan,Wang, Heyao,Sun, Hongbin
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supporting information
p. 2599 - 2604
(2018/07/06)
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- A 2, 6 - difluoro - 4 - bromophenol preparation method (by machine translation)
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The invention relates to a 2, 6 - difluoro - 4 - bromophenol preparation method, the preparation method in order to 3, 5 - difluoro bromobenzene as raw materials, after metalation reaction and oxidation reaction, prepare the high purity of the 2, 6 - difluoro - 4 - bromophenol, the preparation of the synthesizing method of the more inexpensive raw materials, low cost, easy operation, and is suitable for large-scale and continuous production, has very high application prospect. (by machine translation)
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Paragraph 0016; 0028; 0029; 0035; 0036
(2017/06/28)
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- BIARYL DERIVATIVE AS GPR120 AGONIST
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The present invention relates to a biaryl derivative expressed by the chemical formula 1, a method for producing the biaryl derivative, a pharmaceutical composition comprising same, and use of same, the biaryl derivative expressed by the chemical formula 1, as a GPR120 agonist, promoting GLP-1 generation in the gastro-intestinal tract, reducing insulin resistance in the liver, muscles and the like from anti-inflammatory activity in the macrophage, pancreatic cells and the like, and allowing effective use in prevention or treatment of inflammation or metabolic diseases such as diabetes, complications from diabetes, obesity, non-alcoholic fatty liver disease, fatty liver disease, and osteoporosis.
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Paragraph 0101
(2017/11/17)
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- Structure Property Relationships of Carboxylic Acid Isosteres
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The replacement of a carboxylic acid with a surrogate structure, or (bio)-isostere, is a classical strategy in medicinal chemistry. The general underlying principle is that by maintaining the features of the carboxylic acid critical for biological activity, but appropriately modifying the physicochemical properties, improved analogs may result. In this context, a systematic assessment of the physicochemical properties of carboxylic acid isosteres would be desirable to enable more informed decisions of potential replacements to be used for analog design. Herein we report the structure-property relationships (SPR) of 35 phenylpropionic acid derivatives, in which the carboxylic acid moiety is replaced with a series of known isosteres. The data set generated provides an assessment of the relative impact on the physicochemical properties that these replacements may have compared to the carboxylic acid analog. As such, this study presents a framework for how to rationally apply isosteric replacements of the carboxylic acid functional group.
- Lassalas, Pierrik,Gay, Bryant,Lasfargeas, Caroline,James, Michael J.,Tran, Van,Vijayendran, Krishna G.,Brunden, Kurt R.,Kozlowski, Marisa C.,Thomas, Craig J.,Smith, Amos B.,Huryn, Donna M.,Ballatore, Carlo
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p. 3183 - 3203
(2016/05/19)
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- BIARYL DERIVATIVES AS GPR120 AGONISTS
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The present invention relates to biaryl derivatives of Formula 1, a method for preparing the same, a pharmaceutical composition comprising the same and use thereof. The biaryl derivatives of Formula 1 according to the present invention promote GLP-1 formation in the gastrointestinal tract and improve insulin resistance in the liver or in muscle due to anti-inflammatory action in macrophages, lipocytes, etc., and can accordingly be effectively used for preventing or treating diabetes, complications of diabetes, obesity, non-alcoholic fatty liver, steatohepatitis, osteoporosis or inflammation.
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Paragraph 410; 411; 412
(2015/01/16)
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- Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton
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Polo-like kinase (Plk) 1 is a serine-threonine protein kinase that plays a role in cell division, and its overexpression is highly correlated with aggressiveness and prognosis of many cancers. We have designed, synthesized and evaluated a series of terphe
- Mita, Yusuke,Noguchi-Yachide, Tomomi,Ishikawa, Minoru,Hashimoto, Yuichi
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p. 608 - 617
(2013/02/25)
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- NOVEL KINASE MODULATORS
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The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
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Page/Page column 100
(2011/06/10)
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- P-Hydroxyphenacyl photoremovable protecting groups Robust photochemistry despite substituent diversity
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A broadly based investigation of the effects of a diverse array of substituents on the photochemical rearrangement of p-hydroxyphenacyl esters has demonstrated that common substituents such as F, MeO, CN, CO2R, CONH2, and CH3 have little effect on the rate and quantum efficiencies for the photo-Favorskii rearrangement and the release of the acid leaving group or on the lifetimes of the reactive triplet state. A decrease in the quantum yields across all substituents was observed for the release and rearrangement when the photolyses were carried out in buffered aqueous media at pHs that exceeded the ground-state pKa of the chromophore where the conjugate base is the predominant form. Otherwise, substituents have only a very modest effect on the photoreaction of these robust chromophores.
- Givens, Richard S.,Stensrud, Kenneth,Conrad, Peter G.,Yousef, Abraham L.,Perera, Chamani,Senadheera, Sanjeewa N.,Heger, Dominik,Wirz, Jakob
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scheme or table
p. 364 - 384
(2011/06/22)
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- NEW ANALOGS OF POLYSPHORIN AND USES THEREOF FOR TREATING OR PREVENTING MALARIA
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The present invention discloses new analogs of polysphorin and their uses as antimalarial drugs which are highly effective in the hepatic phase of the disease. The present invention further discloses a new method for preparing these compounds.
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Page/Page column 39
(2010/04/28)
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- New oxabispidine compounds for the treatment of cardiac arrhythmias
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There is provided compounds of formula I, wherein R1, R2, R3, R41 to R46, X, Y and Z have meanings given in the description, which compounds are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.
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Page/Page column 54
(2008/06/13)
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- Synthesis and mesomorphic properties of some fluorinated benzoate liquid crystals
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Three series of [4-(4′-n-alkyloxyphenyl)acetylenyl]-2,6- difluorophenyl fluorinated benezoates and one series of fluorinated benzoates with 2,3,5,6-tetrafluorophenylene group and semi-perfluorocarbon chain have been synthesized. Their phase transition temperatures have been measured by texture observation in a polarizing microscope and confirmed by DSC. For the series without fluorocarbon chains, increasing the quantity of fluorosubstituents on the terminal phenyl groups decreased nematic stability (TN-I), but the breadth of the SmA phase range was increased. Lateral fluorosubstitution in the central group lowered the nematic stability (TN-I) and decreased the breadth of the SmA phase range. The series with semiperfluorocarbon chains were more likely to form SmA phases than the series with hydrogencarbon chains, and with the increasing of fluorosubstituents quantity on the terminal phenyl groups nematic and SmA stability (TN-I and TsmA-N) were both decreased.
- Yang, Yong Gang,Chen,Tang,Wen
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- Elemental fluorine Part 12. Fluorination of 1,4-disubstituted aromatic compounds
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Direct fluorination of a series of 1,4-disubstituted benzene derivatives in acid reaction media at convenient temperature leads, in many cases, to selectively fluorinated aromatic products in preparatively useful conversions and yields.
- Chambers, Richard D.,Hutchinson, John,Sparrowhawk, Matthew E.,Sandford, Graham,Moilliet, John S.,Thomson, Julie
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p. 169 - 173
(2007/10/03)
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- Insecticidal ethers
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This invention relates to novel fluorinated ethers, useful as insecticides and acaricides, to processes and intermediates for their preparation, to insecticidal and acaricidal compositions thereof and to methods of combating and controlling insect and acarine pests therewith.
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- Certain 3,5-disubstituted-2-pyridyloxy-fluorophenoxy-alkanoic acids, derivatives thereof and herbicidal properties
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Certain novel fluorophenoxy compounds, principally aryloxyfluorophenoxyalkanoic acids and derivatives thereof, are described. More specifically, these novel compounds bear 1 to 4 fluorine substituents on the phenyl ring. These novel compounds exhibit surprising preemergent and postemergent activity when used according to the method of the invention in the control of grassy weeds.
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- Diphenyl ether derivatives and their use as insecticides
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A compound of formula: STR1 wherein W represents one or more substituents selected from halo, alkyl, alkoxy, alkoxyalkyl, haloalkyl and haloalkoxy or W represents a bidentate group linking adjacent carbon atoms selected from alkylene and alkylenedioxy; Y is a group of formula STR2 wherein X is a group of formula --(CF2)n R3, where R3 is selected from hydrogen, chloro and fluoro, and n is one or two, R1 is selected from hydrogen, chloro, fluoro and hydroxy and R2 is selected from methyl, cyano, ethynyl and hydrogen; Q is selected from carbon bearing a hydrogen atom and nitrogen; and Z represents one or more substituents selected from fluoro, benzyl, phenoxy, chlorophenoxy, fluorophenoxy and bromophenoxy, or any isomer thereof. Processes for preparing these compounds and intermediates for use therein, insecticidal compositions containing these compounds and the use thereof are also disclosed.
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- Insecticidal ethers
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The invention provides insecticidal and acaricidal compounds of formula (I) : wherein X is selected from hydrogen, halo, hydroxy, alkoxy and acyloxy, Z represents a fluoroalkyl group of one or two carbon atoms, Y represents a substituted aryl group where
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