- ALKYNYL ALCOHOLS AS KINASE INHIBITORS
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Selected compounds are effective for prophylaxis and treatment of inflammation and inflammatory disorders, such as NIK-mediated disorders. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, inflammation and the like.
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Page/Page column 47
(2010/01/30)
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- Tautomerism of 5-fluoro-4-hydroxy-2-methoxypyrimidine. Conditions for stabilization of the zwitterionic tautomer
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5-Fluoro-4-hydroxy-2-methoxypyrimidine exists in a solution as two oxo tautomers with the conjugated and isolated double bonds in the ring. The latter tautomer has a zwitterionic structure, and it dominates in water and trifluoroethanol. 5-Fluoro-4-hydroxy-2-methoxypyrimidine in acidic medium gives rise to an equilibrium mixture of two protonated forms at a ratio of about ~1:1. The zwitterionic structure of 4-hydroxypyrimidines is stabilized if the solvent is capable for specific solvation via hydrogen bonding. Pleiades Publishing, Inc., 2006.
- Kheifets,Gindin,Studentsov
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p. 580 - 590
(2007/10/03)
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- NOVEL RING TRANSFORMATION REACTIONS AND THEIR APPLICATIONS TO THE SYNTHESES OF POTENTIAL ANTICANCER HETEROCYCLIC COMPOUNDS
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Novel heterocyclic ring trasformation reactions developed recently in our laboratory are described.They include pyrimidine to pyrimidine, pyrimidine to pyridine transformations.Also discussed are novel one-step procedures for conversion of 1,3-dimethyluracil derivatives into the pyridopyrimidine system.Some applications of these novel reactions to the syntheses of compounds of biological interest are also described.
- Watanabe, K. A.,Su, T.-L.,Pankiewicz, K. W.,Harada, K.
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p. 289 - 307
(2007/10/02)
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- Pyrimidine to pyrimidine transformation process
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There is provided a novel process for pyrimidine to pyrimidine transformations by the displacement of the 1,2,3-portion of a pyrimidine by a 1,3-ambident nucleophile. The novel process requires that the 1 and 3 nitrogens of the pyrimidine moiety be substituted. The novel process makes available, inter alia, novel uracils, simple methods of radioisotopically labeling pyrimidine nuclei, a simple and inexpensive method of preparing the important antiviral and antileukemic material pseudoisocytidine and its new active analog 2'-deoxypseudoisocytidine.
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