87674-15-5Relevant articles and documents
Heteroarylpyrrolopyridinones active as kinase inhibitors
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Page/Page column 17, (2008/06/13)
Compounds represented by formula (I) wherein A, R1, R2, R3, R4, R5 and R6 are as defined in the specification or a pharmaceutically acceptable salt or solvate thereof, compositions thereof,
N-substituted pyrrolopyridinones active as kinase inhibitors
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Page/Page column 18-19, (2010/11/27)
Compounds represented by formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
PYRROLOPYRROLONES ACTIVE AS KINASE INHIBITORS
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Page/Page column 31-32, (2010/11/28)
Compounds represented by formula (I) wherein A, R1, R2, R3, and R4 are as defined in the specification, compositions thereof, and methods of use thereof.
PYRIDYLPYRROLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
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Page/Page column 44, (2010/02/10)
Pyridylpyrrole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treat
REVIEW ON THE METALLATION OF ?-DEFICIENT HETEROAROMATIC COMPOUNDS; REGIOSELECTIVE ORTHO-LITHIATION OF 3-FLUOROPYRIDINE: DIRECTING EFFECTS AND APPLICATION TO SYNTHESIS OF 2,3- OR 3,4-DISUBSTITUTED PYRIDINES
Marsais, Francis,Queguiner, Guy
, p. 2009 - 2021 (2007/10/02)
Metallation of ?-deficient heterocyclic compounds is first reviewed, which shows the important recent developments in this research area.A particular aspect of this reaction is then given with the study of the 3-fluoropyridine metallation regioselectivity.Lithiation of 3-fluoropyridine is chemoselective at low temperatures using butyllithium-polyamine chelates or lithium diisopropylamide.Protophilic attack by these strong bases can be directed either at the 2- or 4-position depending on the lithiation conditions.Various reaction parameters are thus studied such as solvent, temperature, reaction time, lithium-chelating agent as well as metallating agent.The high regioselectivity of 3-fluoropyridine lithiation is theoretically discused, in particular in terms of kinetic of thermodynamic control of the metallation.Chelation between butyllithium and 3-fluoropyridine is proposed, which completely modifies the heterocycle reactivity toward the lithiating agent.This is confirmed by theoretical quantum calculations performed on different models of 3-fluoropyridine using the CNDO/2.These results allow to select the best 3-fluoropyridine-metallation conditions which lead to 3-fluoro-2-lithiopyridine on the one hand and to 3-fluoro-4-lithiopyridine on the other hand.Each of the lithiated isomers is then reacted with a great variety of electrophiles which gives very conveniently the corresponding 2,3- or 3,4-disubstituted pyridines.