- 2-(HETERO)ARYL-BENZIMIDAZOLE AND IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF ASPARAGIME EMETHYL TRANSFERASE
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Substituted benzimidazole and 3H-imidazo[4,5-b]pyridines or formula I: where X and Y respectively are selected from: (i) N and N; and (ii) N and CR4; A2 is selected from:, a C5 heteroarylene group, containing 2 or 3 ring heteroatoms, where the bonds to L1 and the core are β to one another; L1 is selected from: (i)A1-O-CH2-A2; (ii)A1-CH2-O-A2; (iii)A1-C(=O)-NH-A2; (iv)A1-CH(OH)-A2; (v)A1-CH2-NH-C(=O)-A2; (vi) A1-S-CH2-A2; (vii)A1- CH2-S-A2; (viii)A1-CH2-A2; and (ix)A1-CH(CH3)-O-A2; A1 is phenyl, optionally substituted by F or CF3; their use as pharmaceuticals, and in particular, in treating cancer and hemoglobinopathies.
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Page/Page column 115
(2014/09/03)
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- TRICYCLIC COMPOUND
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Provided is a tricyclic compound having a PPAR γ agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4 - R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:
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Page/Page column 84
(2011/06/23)
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- PROCESS FOR THE PREPARATION OF BENZIMIDAZOLES
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The invention provides a process for the preparation of compounds of formula (I) wherein wherein R1 is C1-6-alkyl or C3-6-cycloalkyl, R2 is selected from the group consisting of hydrogen, C1-6-alkyl and C3-6-cycloalkyl, and Q1 is selected from the group consisting of halogen, cyano and -CO-R3, wherein R3 is selected from hydrogen, hydroxy, C1-6-alkoxy, C3-8-cycloalkyloxy, aryloxy, C1-6-alkylamino, aryl-(C1-6-alkyl)amino and di-C1-6-alkylamino, comprising the step of reacting a corresponding o-nitroaniline with an aldehyde R2-CH0 or an equivalent thereof in the presence of a reducing agent.
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Page/Page column 24
(2010/08/08)
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- The nitration of 8-methylquinoxalines in mixed acid
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8-Methylquinoxalines are nitrated surprisingly efficiently at C-5 following a simple nitration protocol with mixed acid at 40-50°C. The implications of halogen functionalisation at C-6 and modification of the mixed acid conditions on the relative rates of conversion and process safety are discussed. Competing side reactions for 6-halo-8-methylquinoxalines involve hydrolysis at C-6 and halogenation at C-7 or C-5.
- Marterer, Wolfgang,Prikoszovich, Walter,Wiss, Jacques,Prashad, Mahavir
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p. 318 - 323
(2013/09/06)
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- Research in 7-aminoindazole series: Synthesis of new halo-7H-4-methylpyrazolo[1,5,4-ef][1,5]benzodiazepin-6-ones and 5H-9-halo-6-methylpyrazolo[1,5,4-ef][1,5]benzodiazepin-4-ones
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A new class of 7-aminohaloindazoles has been synthesized. Reactivity of the amino groups of these bicyclic systems has been investigated. The halogenated pyrazolo-1,5-benzodiazepinones have been synthesized by the condensation of 7-aminoindazoles with ethyl acetoacetate.
- Rakib,Benchidmi,Essassi,El Bouadili,Ibn Mansour,Bellan,Lopez,Lamande
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p. 339 - 345
(2007/10/03)
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- Oxidative Bromination of Aromatic Amides using Sodium Perborate as Oxidant
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Sodium perborate in glacial acetic acid-acetic anhydride with potassium bromide and sodium tungstate as a catalyst, provides a novel system for the bromination of aromatic amides.
- Hanson, James R.,Harpel, Simone,Medina, Inmaculada C. Rodriguez,Rose, Dorian
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p. 432 - 433
(2007/10/03)
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- Catalysts for the Oxidative Bromination of Aromatic Amines and their N-Acetyl Derivatives
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In the nuclear bromination of aromatic amines by bromide and hydrogen peroxide in acetic acid, sodium tungstate has been compared with ammonium molybdate and ammonium vanadate, and found to be an effective catalyst.
- Hanson, James R.,Opakunle, Alexander,Petit, Philippe
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- Heterocyclic Systems Containing Bridgehead Nitrogen Atom : Part XXXVIII- Reaction of 6-Bromo-2-mercapto-4-methylbenzimidazole with Chloroacetic Acid, α-Halogenoketones and 1,2-Dibromoethane
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6-Bromo-8-methylthiazolobenzimidazol-3(2H)-one (IV), 3-substituted-6-bromo-8-methylthiazolobenzimidazoles (VII) and 2,3-dihydro-6-bromo-8-methylthiazolobenzimidazole (VIII) have been synthesized starting from 6-bromo-2-mercapto-4-methylbenzimidazole (II), prepared by the treatment of 5-bromo-3-methyl-1,2-diaminobenzene (I) with carbon disulphide.II on condensation with chloroacetic acid gives 6-bromo-4-methyl-2-benzimidazothiolacetic acid (III) which on cyclization with acetic anhydride furnishes IV and not the other isomer (V).Condensation of II with α-halogenoketones followed by PPA cyclization of the intermediate ketones (VI) yields 3-aryl-6-bromo-8-methylthiazolobenzimidazoles (VII).A similar reaction of II with 1,2-dibromoethane gives VIII.
- Gupta, G. D.,Gupta, Rakesh P.,Pujari, H. K.
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p. 1035 - 1037
(2007/10/02)
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