- Synthesis of 6,6'-diamino-2,2'-biquinoline and 2,2'-bi-1,6- naphthyridine
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High-yield synthesis and characterization of the new heterocycles 6,6'- diamino-2,2'-biquinoline (3), 6,6'-bis(N,N-dimethyl-amino)-2,2'-biquinoline (4), and 2,2'-bi-1,6-naphthyridine (5) are described. The preparation of 3 and 4 is based on the coupling of 2-amino-6-chloroquinoline and 2-chloro-6- dimethylaminoquinoline in the presence of NiCl2·6H2O/PPh3/Zn in DMF (NiCRA). Compound 5 was synthesized through a condensation reaction of 4- aminopyridine-3-carbaldehyde and butane-2,3-dione.
- Janiak, Christoph,Deblon, Stephan,Uehlin, Lars
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Read Online
- Ugi three-component reaction of alcohols, amines and isocyanides: A new approach to the synthesis of cyclic amidines
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We have developed a novel, simple, efficient and one pot synthetic protocol for the synthesis of cyclic amidines via Ugi three-component reaction of alcohols, amines, and isocyanides.
- Dev, Kapil,Ramakrishna,Maurya, Saransh Wales,Siddiqui, Ibadur Rahman,Kant, Ruchir,Maurya, Rakesh
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supporting information
p. 1202 - 1206
(2017/03/02)
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- SUBSTITUTED HETEROCYCLIC AZA DERIVATIVES
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The invention relates to heterocyclic aza derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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- Substituted Heterocyclic Aza Compounds
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Heterocyclic aza compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds and also methods of using these compounds for the treatment and/or inhibition of pain and further diseases and/or disorders.
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- Kinase inhibitors
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Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
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- Kinase inhibitors
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Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
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Page/Page column 24
(2010/01/31)
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- 4-Aminopyridine derivatives with antiamnesic activity
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Acetylcholine (Ach) enhancement, useful in the treatment of Alzheimer's disease (AD), may be obtained by means of ion channel modulators such as 4- aminopyridine (4-AP). 4-AP is also the central ring of tacrine, the first drug approved for the treatment of AD. The synthesis and pharmacological activity of three 4-AP derivatives, prepared with the aim of improving their antiamnesic activity, is here described. In two of these compounds 4-AP is connected to 4-aminobutyric acid (GABA), whereas in the third it is connected to 2-indolinone, i.e., the skeleton of linopirdine, another Ach enhancing agent. The new compounds showed potent antiamnesic activity in comparison with piracetam. (C) 2000 Edition scientifiques et medicales Elsevier SAS.
- Andreani, Aldo,Leoni, Alberto,Locatelli, Alessandra,Morigi, Rita,Rambaldi, Mirella,Pietra, Claudio,Villetti, Gino
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- Regiospecific Electrophilic Substitution of Aminopyridines: Ortho Lithiation of 2-, 3-, and 4-(Pivaloylamino)pyridines
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2- and 4-(pivaloylamino)pyridines have been shown to undergo metalation exclusively at C-3 and these smoothly react with a variety of electrophiles to produce 2,3- and 3,4-disubstituted pyridines, respectively.Removal of the pivaloyl protecting group results in overall electrophilic substitution of an aminopyridine.Utilization of this method is exemplified by efficient syntheses of 2- and 4-aminonicotinaldehydes.Minor modifications of the reaction conditions permitted exclusive ortho metalation of 2-(pivaloylamino)pyridines additionally functionalized by chloro, fluoro, or methyl groups.Although the major product from reaction of 3-(pivaloylamino)pyridine by this method was metalation at C-4, the reaction was complicated by substantial quantities of product derived from nucleophilic attack by n-butyllithium on the pyridine nucleus.
- Turner, James A.
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p. 3401 - 3408
(2007/10/02)
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