- Azaindole synthesis through dual activation catalysis with N-heterocyclic carbenes
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A convergent, transition-metal-free synthesis of 2-aryl-azaindoles has been developed. The interception of a reactive aza-ortho-azaquinone methide intermediate by an acyl anion equivalent generated through carbene catalysis provides high yields, a wide substrate scope, and the synthesis of previously inaccessible azaindoles.
- Sharma, Hayden A.,Todd Hovey,Scheidt, Karl A.
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supporting information
p. 9283 - 9286
(2016/07/25)
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- An efficient one-pot synthesis of 2-bromo-6-aryl[5H]pyrrolo[2,3-b]pyrazines
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We report a two step one-pot method for the synthesis of 2-bromo-6-aryl[5H]pyrrolo[2,3-b]pyrazines. The process makes use of a cleaner copper-free Sonogashira coupling and an improved base-mediated 5-exo-dig cyclisation to afford the products in good yields. This method expands the scope to structures that are poorly represented in the literature and incorporates a halide for further synthetic elaboration.
- Simpson, Iain,St-Gallay, Steve A.,Stokes, Stephen,Whittaker, David T.E.,Wiewiora, Rafal
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p. 1492 - 1495
(2015/03/14)
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- AMIDE DERIVATIVES AND DRUGS
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The present invention provides an amide derivative represented by the following formula [1]: wherein n represents 0 or 1; X represents CR4 or N; Y represents CR6 or N; Z represents CR7 or N; R1 and R2 may be the same or different and each represents hydrogen, optionally substituted alkyl, acyl, optionally substituted aryl, or an optionally substituted aromatic heterocyclic group; R4, R5, R6 and R7 may be the same or different and each represents hydrogen, halogen, hydroxy, amino, alkyl, haloalkyl, alkoxy, monoalkylamino, dialkylamino, arylalkyl, cyano, or nitro; and R3 represents optionally substituted alkylamino, optionally substituted arylamino, or optionally substituted cyclic amino, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising them as an active ingredient. The compound of the present invention is useful as a TGF-β inhibitor.
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- 6-Substituted-5H-pyrrolo[2,3-b]pyrazines via palladium-catalyzed heteroannulation from N-(3-chloropyrazin-2-yl)-methanesulfonamide and alkynes
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We herein report the efficient and convenient synthesis of 6-substituted-5H-pyrrolo[2,3-b]pyrazines. The reaction is a palladium-catalyzed heteroannulation process followed by deprotection to yield the desired pyrrolo[2,3-b]pyrazine substrates. The reacti
- Hopkins, Corey R.,Collar, Nicola
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p. 8087 - 8090
(2007/10/03)
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- An improved method for the synthesis of 6-substituted-5H-pyrrolo[2,3-b] pyrazines via palladium-catalyzed heteroannulation using microwave heating
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We herein report an improved synthesis of 6-substituted-5H-pyrrolo[2,3-b] pyrazines utilizing microwave heating. The reaction is a palladium-catalyzed heteroannulation process followed by deprotection to yield the desired substrates in good yield.
- Hopkins, Corey R.,Collar, Nicola
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p. 8631 - 8633
(2007/10/03)
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- Pyrrolopyrazines as kinase inhibitors
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The invention relates to pyrrolo [2,3b]-pyrazine derivatives having the general formula (I) : ???wherein :R2 and R3 are identical or different and represent H, C1-C6 alkyl, said alkyl being a straight or branched-chain alkyl, which can be substituted,R6 i
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- Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects
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Cyclin-dependent kinases (CDKs) regulate the cell cycle, apoptosis, neuronal functions, transcription, and exocytosis. The observation of CDK deregulations in various pathological situations suggests that CDK inhibitors may have a therapeutic value. In th
- Mettey, Yvette,Gompel, Marie,Thomas, Virginie,Garnier, Matthieu,Leost, Maryse,Ceballos-Picot, Irène,Noble, Martin,Endicott, Jane,Vierfond, Jean-Michel,Meijer, Laurent
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p. 222 - 236
(2007/10/03)
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- Reactions of β-(lithiomethyl)azines with nitriles as a route to pyrrolo-pyridines, - quinolines, -pyrazines, - quinoxalines and -pyrimidines
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Deprotonation of 3-methylazines, followed by reaction with benzonitile, gives an intermediate which, on treatment with additional strong base, cyclises to give 2-phenyl[1H]-pyrrolo[2,3-b]pyridine. The application of this type of reaction to a variety of n
- Davis, Michael L.,Wakefield, Basil J.,Wardell, Jacklyn A.
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p. 939 - 952
(2007/10/02)
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- Cyclisation par amination intramoleculaire dans la serie de la pyrazine.
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An original one-pot synthesis of 4,7-diazaindoles is achieved by metalation of methylpyrazines or methylquinoxaline which are then condensed with an aromatic nitrile : an intermediate imine-enamine is formed which leads, by intramolecular cyclization, to diazaindoles.
- Vierfond, Jean-Michel,Mettey, Yvette,Mascrier-Demagny, Line,Miocque, Marcel
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p. 1219 - 1222
(2007/10/02)
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