- One-pot, pseudo five-component synthesis of spirooxindole derivatives containing fused 1,4-dihydropyridines in water
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An efficient, facile, and simple route for the preparation of spirooxindole-containing fused 1,4-dihydropyridine derivatives through a one-pot, pseudo five-component condensation reaction of isatin or its derivatives, 1,1-bis(methylthio)-2-nitroethylene, 1,3-dicarbonyl compounds, and two equivalents of ammonia in water is reported. The merits of this method include the use of water as a green solvent, and inexpensive and easily available starting materials and catalyst, the high yield of products, and the straightforward work-up. Georg Thieme Verlag Stuttgart · New York.
- Alizadeh, Abdolali,Mikaeili, Azadeh,Firuzyar, Tahereh
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experimental part
p. 1380 - 1384
(2012/06/30)
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- Heterocyclic Compounds Useful as RAF Kinase Inhibitors
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The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
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Page/Page column 46
(2009/01/24)
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- COMPOUNDS USEFUL AS RAF KINASE INHIBITORS
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The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.
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Page/Page column 91
(2009/03/07)
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- PYRIDO PYRIMIDINONES, DIHYDRO PYRIMIDO PYRIMIDINONES AND PTERIDINONES USEFUL AS RAF KINASE INHIBITORS
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The present invention provides compounds having the formula: (I) wherein A-B together represents one of the following structures; (II), (III), (IV) and n, R1, R2, R3, R4, L1, L2, Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., RAF), and thus are useful, for example, for the treatment of RAF mediated diseases.
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Page/Page column 105
(2010/11/08)
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- Innovative approaches to the imidazo[4,5-b]pyridine ring system. Development of an efficient process for industrial-scale production of a key intermediate for potent angiotensin II receptor antagonists
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Two syntheses of 2-ethyl-5,7-dimethyl-3H-imidazo[4,5-b]pyridine (3), an important intermediate for the synthesis of several potent angiotensin II antagonists, have been investigated. The first route involves conversion of 1,1-bis(methylthio)-2-nitroethene (17) to 2-ammo-4,6-dimethyl-3-nitropyridine (6); catalytic hydrogenation of 6 in propionic acid gave 3 in high yield. In the second synthesis, propionitrile is converted to imidate hydrochloride 15·HCl which is neutralised and reacted with aminoacetonitrile in the presence of acetylacetone to give 3 in 55% overall yield. The propionitrile route was scaled up to produce 3 in the pilot plant.
- Stucky, Gerhard C.,Roduit, Jean-Paul,Schmidt, Beat
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p. 280 - 282
(2007/10/03)
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- Polyfunctional pyridines from nitroacetamidine and β-diketones. A useful synthesis of substituted imidazo[4,5-b]pyridines and related compounds
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Nitroacetamidine undergoes a useful cyclocondensation with β-diketones to produce substituted 2-amino-3-nitropyridines. Use of an acylpyruvate generates hitherto unreported 2-amino-3-nitropyridine-4-carboxylates. These may be converted easily to functionalized imidazo[4,5-b]pyridines and oxazolo[5,4-b]pyridines.
- Batt,Houghton
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p. 963 - 969
(2007/10/02)
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