95740-49-1Relevant articles and documents
Micro reaction system and method for synthesizing 4-bromo-3-methylanisole through two-phase method
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Paragraph 0016; 0027, (2019/01/16)
The invention discloses a micro reaction system and method for synthesizing 4-bromo-3-methylanisole through a two-phase method, and belongs to the technical field of chemical engineering. The micro reaction system comprises a micro mixer, a micro packed b
Transition-metal-free decarboxylative bromination of aromatic carboxylic acids
Quibell, Jacob M.,Perry, Gregory J. P.,Cannas, Diego M.,Larrosa, Igor
, p. 3860 - 3865 (2018/04/26)
Methods for the conversion of aliphatic acids to alkyl halides have progressed significantly over the past century, however, the analogous decarboxylative bromination of aromatic acids has remained a longstanding challenge. The development of efficient methods for the synthesis of aryl bromides is of great importance as they are versatile reagents in synthesis and are present in many functional molecules. Herein we report a transition metal-free decarboxylative bromination of aromatic acids. The reaction is applicable to many electron-rich aromatic and heteroaromatic acids which have previously proved poor substrates for Hunsdiecker-type reactions. In addition, our preliminary mechanistic study suggests that radical intermediates are not involved in this reaction, which is in contrast to classical Hunsdiecker-type reactivity. Overall, the process demonstrates a useful method for producing valuable reagents from inexpensive and abundant starting materials.
IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS HISTONE DEMETHYLASE INHIBITORS
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Paragraph 0198-0199, (2018/01/15)
This disclosure relates, inter alia, to compounds that inhibit histone demethylase activity. In particular, the disclosure relates to compounds that inhibit histone lysine demethylase KDM5B, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions disclosed herein.
Electronic influences in phosphinesulfonato palladium(II) polymerization catalysts
Wucher, Philipp,Goldbach, Verena,Mecking, Stefan
supporting information, p. 4516 - 4522 (2013/09/23)
To study the influence of electronics on catalytic polymerization properties independent from sterics, phosphinesulfonato Pd(II) complexes bearing remotely located substituents on the nonchelating P-bound aryls [κ2-(P,O)-(4-R-2-anisyl)2PC6H 4SO2O]Pd(Me)(dmso) (1a-e-dmso: 1a, R = CF3; 1b, R = Cl; 1c, R = H; 1d, R = CH3; 1e, R = OCH3) were prepared. The electron-poor complex 1a-dmso (4-CF3) undergoes the fastest insertion of methyl acrylate (MA) and is the most active for ethylene polymerization. The polyethylene molecular weight increases by a factor of 2 for the more electron rich complex 1e-dmso (4-OCH3) (Mn = 17 × 103 vs 8 × 103 for 1a-dmso (4-CF 3)). MA/ethylene copolymerization experiments revealed that the MA incorporation ratio and copolymer molecular weights are largely independent of the electronic nature of the remote substituents. These trends were further confirmed by studies of two mixed P-aryl/-alkyl complexes 1f-dmso ([κ2-(2,4,6-(OMe)3C6H2)( tBu)PC6H4SO2O]Pd(Me)(dmso)) and 1g-dmso ([κ2-(C6H5)(tBu) PC6H4SO2O]Pd(Me)(dmso)). In ethylene/MA copolymerization, 1f-dmso affords a significantly higher molecular weight polymer with reasonable MA incorporation (Mn = 12 × 10 3 and 7.7 mol % MA) and activities similar to those observed for complexes 1a-e-dmso.
NOVEL ANTIVIRAL COMPOUNDS
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, (2013/02/27)
The present invention relates to compounds of formula (A) as defined herein having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
NOVEL VIRAL REPLICATION INHIBITORS
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, (2011/02/24)
The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
Discovery of 6-aryl-7-alkoxyisoquinoline inhibitors of IκB kinase-β (IKK-β)
Christopher, John A.,Bamborough, Paul,Alder, Catherine,Campbell, Amanda,Cutler, Geoffrey J.,Down, Kenneth,Hamadi, Ahmed M.,Jolly, Adrian M.,Kerns, Jeffrey K.,Lucas, Fiona S.,Mellor, Geoffrey W.,Miller, David D.,Morse, Mary A.,Pancholi, Kiritkant D.,Rumsey, William,Solanke, Yemisi E.,Williamson, Rick
supporting information; experimental part, p. 3098 - 3102 (2010/03/03)
The identification and progression of a potent and selective series of isoquinoline inhibitors of IκB kinase-β (IKK-β) are described. Hit-generation chemistry based on IKK-β active-site knowledge yielded a weakly potent but tractable chemotype that was rapidly progressed into a series with robust enzyme and cellular activity and significant selectivity over IKK-α.
BI- OR TETRA-GUANIDINO-BIPHENYL COMPOUNDS AS SMALL MOLECULE CARRIERS
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, (2008/06/13)
The invention relates to compounds of formula: I, or pharmaceutically acceptable a salts thereof, I wherein X1 X2 and X3 are each independently where Y is an alkylene, alkenylene or alkynylene group, each of which may be optionally substituted with one or more substituents selected from alkyl, halo, CF3, OH, alkoxy, NH2, CN, NO2 and COOH; W is absent or is O, S or NH; Rl, R2, R3 and R4 are each independently selected from H, alkyl, aryl and a protecting group Pl; R7, R8 and R9 are each independently selected from H, alkyl, halo, CF3, OH, alkoxy, NH2, CN, NO2 and COOH; q and r are each independently 1, 2, 3 or 4; q' and r' are each independently 0, 1, 2 or 3, where q + q' and r + r' each equal 4; p is 1, 2, 3, 4 or 5, and p' is 0, 1, 2, 3 or 4, where p + p' is 5; n is 0, 1, 2, 3....6; L is (Z)mNR5R6 where Z is a hydrocarbyl group and m is 0 or 1; where R5 and R6 are each independently H, CO(CH2)jQ1 or C=S(NH)(CH2)kQ2 where j and k are each independently 0, 1, 2, 3, 4 or 5, and Q1 and Q2 are each independently selected from COOH, a chromophore or R5, R6 and the nitrogen to which they are attached together form.
Synthesis of (±) curcuphenol and (±)-β-sesquiphellandrene
Sharma,Chand, Tek
, p. 553 - 556 (2007/10/03)
Two naturally occurring compounds curcuphenol 1 and β-sesquiphellandrene 2 have been synthesised using lithium tetrachlorocuperate catalysed coupling reaction.