- Rapid and efficient synthesis of [18F]fluoronicotinamides, [18F]fluoroisonicotinamides and [18F]fluorobenzamides as potential pet radiopharmaceuticals for melanoma imaging
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In an attempt to simplify nucleophilic radiofluorination reactions to be amenable for automation, a series of [18F]fluoronicotinamides, [ 18F]fluoroisonicotinamides and [18F]fluorobenzamides were synthesized using one-step
- Al Jammaz,Al-Otaibi,Okarvi,Amartey
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scheme or table
p. 312 - 317
(2012/06/04)
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- Microwave-assisted synthesis of substituted fluoroazines using KF·2H2O
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This Letter describes a new microwave-assisted fluorination of azines using hydrated potassium fluoride in untreated DMSO under atmospheric conditions. It is thought that microwave irradiation promotes desolvation of the fluorine anion leading to halide n
- Shestopalov, Anatoliy M.,Fedorov, Alexander E.,Rodinovskaya, Liudmila A.,Shestopalov, Alexander A.,Gakh, Andrei A.
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experimental part
p. 5257 - 5259
(2009/12/06)
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- JNK INHIBITOR
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The present invention relates to a c-Jun N-terminal kinase inhibitor containing an azole compound (I) substituted by a nitrogen-containing aromatic group having substituent(s)(except a compound represented by the formula: ) or a salt thereof or a prodrug thereof.
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Page/Page column 80
(2010/02/07)
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- Bis-acyloxymethyl derivatives
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This invention relates to new pyridyl, quinoline and acridine bis-acyloxymethyl compounds; to compositions comprising these compounds; and to processes for their utility as fungicides, bactericides and as inhibitors of the growth of cancer in warm-blooded animals. In accordance with this invention, new bis-acyloxymethyl derivatives are provided of the formula: STR1 wherein B is selected from substituted and unsubstituted alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl and alkynyl; A is selected from hydrogen and B; or, A and B together comprise a pyrrolizine; L is selected from STR2 wherein Y is selected from hydrogen or STR3 each R and Z is independently selected from hydrogen or substituted and unsubstituted alkyl, cycloalkyl, aryl, alkenyl, cycloalkenyl, alkynyl, amine group, each Z' is independently selected from hydrogen and substituted or unsubstituted alkyl; M is Z or is selected from halogen, nitro, hydroxyl, nitrile and substituted or unsubstituted, carboxylic acid group, carboxylic acid ester group, carboxylic acid amide group, sulfonic acid group and sulfonic acid amide group; ether group, thioether group, acylated hydroxyl, sulfonylamide, sulfonylurea, sulfoxide group, sulfone group and mixtures thereof; each n is the same and is 0 or 1; q is from 0-4; and, X is the anion of an acid.
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- Carboxamidation of pyridines by the system of elemental fluorine- carbonitrile-water: A useful alternative to the chichibabin amination
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The title reaction with pyridine, 4-methylpyridine, 3-methylpyridine, 3- bromopyridine, nicotinonitrile, and quinoline yields 2-carboxamido derivatives regioselectively. Isoquinoline is amidated at position 1.
- Kiselyov,Strekowski
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p. 2387 - 2392
(2007/10/02)
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- Synthesis, Chemistry, and Antineoplastic Activity of α-Halopyridinium Salts: Potential Pyridone Prodrugs of Acylated Vinylogous Carbinolamine Tumor Inhibitors
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A series of 4- and 5-methyl>-1H-pyrrolizin-5-yl>-2-halopyridinium iodides were synthesized.The rates of hydrolysis of the α-halopyridinium salts to the corresponding pyridones, and the reactivities of the carbamate moieties were studied as a function of pH, buffer composition, and ionic strength.The 4- and 5-pyrrolizinyl-2-halopyridinium iodides and the corresponding pyridones were evaluated against P388 lymphocytic leukemia in vivo.The α-fluoropyridinium compounds were active but the α-chloro compounds were not.This activity was correlated with the rates of hydrolysis of the α-halopyridinium compounds to the active pyridone.Compounds that were active in the P388 screen were evaluated in L1210 leukemia, M5076 carcinoma, and MX-1 mammary xenograft assays in mice.
- Anderson, Wayne K.,Dean, Dennis C.,Endo, Toshiyasu
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p. 1667 - 1675
(2007/10/02)
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- Preparation of 2-Fluoropyridines via Base-Induced Decomposition of N-Fluoropyridinium Salts
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N-Fluoropyridinium salts with either BF4-, SbF6-, or PF6- as a counteranion were treated with excess base such as triethylamine at room temperature to give 2-fluoropyridine in good yield.This method was succesfully applied to the preparation of 2-fluoropyridine derivatives possessing electron-donating or -withdrawing substituents using substituted N-fluoropyridinium tetrafluoroborates.Pyridine-F2 compounds produced through reactions of pyridines with molecular fluorine were also treated with base to give 2-fluoropyridines but in low yields.These reactions are considered to occur through a carbene mechanism as follows: a novel N-F-containing cyclic carbene (3), generated from the N-fluoropyridinium salts by 2-proton abstraction, reacts with fluorine atoms from counteranions such as BF4-, SbF6-, or PF6-, followed by elimination of F- from the N-F moiety, to yield 2-fluoropyridines.Previously reported findings in reactions of pyridines with molecular fluorine are explained on the basis of this mechanism.
- Umemoto, Teruo,Tomizawa, Ginjiro
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p. 1726 - 1731
(2007/10/02)
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- DIRECT FLUORINATION OF SUBSTITUTED PYRIDINES
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The direct fluorination of pyridines bearing alkyl, halogen, ester, or ketone functions has been employed to prepare the corresponding 2-fluoro-substituted pyridines.
- Puy, Michael Van Der
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p. 255 - 258
(2007/10/02)
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