- Microwave fluorination: A novel, rapid approach to fluorination with Selectfluor
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Fluorination of electron rich aromatic systems with electrophilic fluorination reagents such as Selectfluor and Accufluor is a well-established process. Herein we report results from investigations into the use of such procedures to perform rapid, small-scale fluorinations under microwave irradiation. We have investigated the transformation with a range of different substrates and discuss the effects of two key factors, namely reaction time and choice of fluorination reagent. The use of Selectfluor in acetonitrile at 150°C with microwave heating for 10 min affords products in comparable yields to those obtained by prolonged heating in acetonitrile at its reflux temperature.
- Bluck, Gavin W.,Carter, Neil B.,Smith, Stephen C.,Turnbull, Michael D.
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- NUCLEOPHILIC DISPLACEMENT IN POLYHALOGENAROMATIC COMPOUNDS. PART 12. ADDITIVITY OF FUORINE SUBSTITUENT EFFECTS IN METHOXYDEFLUORINATION
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The rates of methoxydefluorination of all twelve polyfluorobenzenes in dimethyl sulphoxide-methanol mixtures (DMSO-MeOH; 9:1 v/v; 298.2 K) have been measured.Three substituent rate factors (Fo, 60; fm, 180; fp, 0.75) are sufficient to reproduce the effect of the fluorine substituent in this reaction upon each member of the series.The solvent effect, comparing these results with an earlier and more limited study in methanol is predominantly a simple acceleration.The effects of substituents upon the rate of methoxydefluorination of fuorobenzene itself are slightly greater(ρ-, 6.9) than in the corresponding reaction of pentafluorobenzene derivatives (ρ-, 5.8) but the change in sensitivity is much less than that found with nitrobenzene derivatives.
- Bolton, R.,Sandall, J. P. B.
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- Synthesis technology of 2,3-difluorophenol
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The invention relates to a synthesis technology of 2,3-difluorophenol. 1,2,3-trifluoro-benzene is used as a raw material, and 2,3-difluorophenol is prepared through oxyalkylation and dealkylation reactions. The synthesis route is short, the technology operation is simple, special equipment is not needed, the yield reaches 82% or above, and the synthesis technology has good industrial prospects.
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Paragraph 0015; 0029-0030; 0032-0033; 0035-0036
(2018/10/11)
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- Glucopyranosyl derivative and application thereof in medicines
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The invention relates to a glucopyranosyl derivative used as a sodium-dependent glucose transporter (SGLT) inhibitor, a medicinal composition containing the derivative, and an application of the derivative and the medicinal composition in medicines, and especially relates to the glucopyranosyl derivative represented by formula (I) or a pharmaceutically acceptable salt or all stereoisomers thereof, or the medicinal composition containing the derivative, and a use of the derivative and the medicinal composition in the preparation of medicines for treating diabetes and diabetes related diseases.
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Paragraph 0528; 0530; 0531; 0532; 0533
(2016/10/08)
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- GLUCOPYRANOSYL DERIVATIVES AND THEIR USES IN MEDICINE
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Disclosed are glucopyranosyl derivatives used as sodium dependent glucose cotransporters (SGLTs) inhibitors, intermediates or preparation processes thereof, and pharmaceutical uses thereof, especially glucopyranosyl derivatives represented by Formula (I), or pharmaceutically acceptable salts or all stereoisomers thereof, pharmaceutical compositions containing these derivatives and their uses for treatment of diabetes and diabetes-related diseases.
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Paragraph 00226
(2015/04/15)
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- Halogenated analogs of 1′-acetoxychavicol acetate, Rev-export inhibitor from Alpinia galanga, designed from mechanism of action
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In the course of search for the robust analogs of 1′-acetoxychavicol acetate (ACA, 1), the Rev-export inhibitor from the medicinal plant Alpinia galanga, we clarified formation of the quinone methide intermediate ii to be essential for exerting the inhibi
- Tamura, Satoru,Shiomi, Atsushi,Kimura, Tominori,Murakami, Nobutoshi
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scheme or table
p. 2082 - 2085
(2010/07/05)
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- Cycloalkyl alkanoic acids as integrin receptor antagonists derivatives
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The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αvβ3 and/or αvβ5 integrin.
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- Cycloalkyl alkanoic acids as integrin receptor antagonists derivatives
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The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αvβ3 and/or αvβ5 integrin.
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- Synthesis and anticancer activity of fluorinated analogues of combretastatin A-4
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The synthesis of a series of fluorinate d benzaldehydes and their use in the Wittig synthesis of fluoro-substituted stilbenes is described. 3,5-Difluoro-4-hydroxybenzaldehyde (6) and 3-fluoro-4-methoxybenzaldehyde (11) are prepared by Duff formylation of 3,5-difluorophenol and 2-fluoroanisole, respectively. 2-Methoxy-3,4-difluorobenzaldehyde was obtained by Friedel-Crafts formylation of 2,3-difluoroanisole with α,α-dichloromethyl methyl ether. The aldehydes were used to make a series of fluorinated analogues of the anticancer combretastatins A-1, A-2 and A-4. The in vitro anticancer properties of the fluoro combretastatins are reported. The most active fluoro analogue 3-deoxy-3-fluoro-combretastatin A-4 (Z-2) retains the potent cell growth inhibitory properties of CA-4.
- Lawrence, Nicholas J.,Hepworth, Lucy A.,Rennison, David,McGown, Alan T.,Hadfield, John A.
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p. 101 - 108
(2007/10/03)
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- 2-AMINOTETRALINES AND PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND THERAPEUTIC TREATMENT OF INFLAMMATORY AND/OR AUTOIMMUNE PATHOLOGIES
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2-Aminotetralines, a process for their preparation, and pharmaceutical compositions. for the prevention and therapeutic treatment of inflammatory pathologies (particularly septic shock) and/or autoimmune pathologies in which the aetiopathogenic role of in
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- Process for generating electrophiles from anions by reaction with electrophilic fluorinating agent
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A process includes substituting a substituent on a substrate. The process includes reacting a salt of an anionic form of the substituent with an electrophilic fluorination agent to provide an electrophile containing a cationic form of the substituent. The electrophile is then electrophilically substituted on the substrate. In some aspects of the process, the substrate can be an aromatic or a non-aromatic. The process can be used for a variety of reactions having electrophilic mechanisms, including halogenation, thiocyanation and nitration.
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- An unexpected route to fluorinated anisoles
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We found a new one-pot procedure for the synthesis of polyfluoroanisoles from polyfluoroanilines. The reaction involves aromatic nucleophilic substitution of o- or p-fluorine of benzenediazonium salt with methoxy group followed by reductive removal of the diazonium group.
- Takechi, Naoto,Fukai, Yasushi,Oka, Kazuyoshi,Huisgen, Rolf
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