- INHIBITORS OF INFLUENZA VIRUS REPLICATION AND USES THEREOF
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The invention provides a class of compounds as inhibitors of influenza virus replication, preparation methods thereof, pharmaceutical compositions containing these compounds, and uses of these compounds and pharmaceutical compositions thereof in the treatment of influenza.
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Paragraph 00413
(2018/07/05)
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- Cu-catalyzed fluorination of diaryliodonium salts with KF
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A mild Cu-catalyzed nucleophilic fluorination of unsymmetrical diaryliodonium salts with KF is described. This protocol preferentially fluorinates the smaller aromatic ligand on iodine(III). The reaction exhibits a broad substrate scope and proceeds with high chemoselectivity and functional group tolerance. DFT calculations implicate a CuI/CuIII catalytic cycle.
- Ichiishi, Naoko,Canty, Allan J.,Yates, Brian F.,Sanford, Melanie S.
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supporting information
p. 5134 - 5137
(2013/10/22)
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- Cascade iodination-fluorination synthesis of 2-fluorothiophene and 5-fluoro-2-thienyliodonium salts
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The first synthesis of fluorine-containing 2-thienyliodonium salts was accomplished using cascade iodination-fluorination. According to this methodology, thiophene is first converted to bis(2-thienyl)iodonium hexafluorophosphate using an electrophilic iodination reaction. Upon heating with potassium fluoride, this salt undergoes regioselective fluorination producing 2-fluorothiophene. 2-Fluorothiophene is then iodinated again to yield fluorothienyliodonium salts.
- Onys'ko, Petro P.,Kim, Tetyana V.,Kiseleva, Olena I.,Rassukana, Yuliya V.,Gakh, Andrei A.
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body text
p. 501 - 504
(2010/01/14)
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- 1,2,4-TRIAMINOBENZENE DERIVATIVES USEFUL FOR TREATING DISORDERS OF THE CENTRAL NERVOUS SYSTEM
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The present invention concerns 1,2,4-triaminobenzene derivatives of the general formula I or pharmaceutically acceptable salts thereof and the use thereof.
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- THE FLUORINATION OF SIMPLE FIVE-MEMBERED HETEROAROMATIC COMPOUNDS WITH ELEMENTAL FLUORINE
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The reaction of elemental fluorine with five-membered heteroaromatics under controlled conditions proceeds cleanly, yielding major substitution products in the case of thiophene (1) and N-methylpyrrole (2) or 1,4-addition products in the case of furan (3), while pyrrole (4) gives only tars.The site of fluorine substitution on N-methylpyrrole remarkably favours the β carbon atoms by a factor of ca. 3 over the α carbons.The α/β substitution ratio for 1 (1.9) and 2 (0.28) and the intermolecular reactivity order N-methylpyrrole > thiophene > benzene agrees with a polar electrophilic substitution mechanism.Also the predominantly syn 1,4-addition to furan conforms to the polar syn addition of F2 to double bonds.
- Cerichelli, Giorgio,Crestoni, Maria Elisa,Fornarini, Simonetta
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p. 749 - 755
(2007/10/02)
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- DIRECT FLUORINATION OF THIOPHENE AND N-METHYLPYRROLE
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The reaction of thiophene and N-methylpyrrole with elemental fluorine under carefully controlled conditions affords a direct way of introducing a single fluorine atom into the 2- or 3-position of the five-membered rings.
- Crestoni, Maria Elisa,Fornarini, Simonetta
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p. 203 - 204
(2007/10/02)
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- Electrophilic Fluorination with N-Fluoroquinuclidinium Fluoride
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N-Fluoroquinuclidinium fluoride (NFQNF), obtainable in ca. 90percent yield by direct low-temperature liquid-phase fluorination of quinuclidine, has been used to deliver 'positive' fluorine to carbanionic sites in a number of organic substrates.
- Banks, R. E.,Boisson, R. A. Du,Tsiliopoulos, E.
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p. 461 - 466
(2007/10/02)
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- Kinetics of Bromination of Certain Substituted Thiophenes in Solution
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The general features of the kinetics of bromination of thiophene and substituted thiophenes have been investigated in dry and 15percent aq. acetic acid (v/v) and the Arrhenius activation energy (Ea) accurately determined for ten thiophene derivatives and interpreted.The mechanism proposed is supported with the detection of a ?-complex between bromine and 2-bromothiophene.
- Kannappan, V.,Nanjan, M. J.,Ganesan, R.
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p. 1183 - 1187
(2007/10/02)
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- Sulfonation of aromatic compounds in the presence of solvents
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A process for the sulfonation of aromatic compounds wherein an aromatic substance consisting of one or more aromatic compounds susceptible to the action of sulfur trioxide is formed into a reactant by admixture with one or more organic liquids, substantially inert to sulfur trioxide under the conditions of the process, which reactant is brought to boiling at a temperature not greater than 100° C under a pressure of from 0.1 mm Hg to atmospheric pressure, gaseous sulfur trioxide is introduced thereinto thereby causing it to continue to boil, the component or components of the reactant thus volatilized is or are reconverted to liquid in a heat-exchanger and recycled to the reaction chamber, and the pressure in the reaction chamber and the rate at which the gaseous sulfur trioxide is introduced into the reactant are controlled so as to ensure that there is always present in the reaction chamber an amount of volatilizable matter exceeding that amount volatilizable by the heat of reaction of the aromatic substance present in the reaction chamber with the gaseous sulfur trioxide in contact with said aromatic substance and that the temperature of the reaction mixture is a temperature of 100° C or below.
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