- USE OF FLUORINATED DERIVATIVES OF 4-AMINOPYRIDINE IN THERAPEUTICS AND MEDICAL IMAGING
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The present disclosure provides novel compounds, including compounds that bind to potassium channels, methods for their manufacture, and methods for their use, including for the treatment of demyelinating diseases and/or in vivo imaging of the central nervous system to diagnose and/or assess the progression of MS or other diseases.
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Paragraph 00199
(2013/12/03)
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- HETEROCYCLIC KINASE INHIBITORS
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Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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- Configurationally Stable Biaryl Analogues of 4-(Dimethylamino)pyridine: A Novel Class of Chiral Nucleophilic Catalysts
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A short synthetic approach toward a novel class of chiral nucleophilic catalysts, the dissymmetry of which stems from restricted rotation about an Ar-Ar bond, has been developed. The key steps of the synthesis include preparation of a nucleophilic 1-methyl-2-pyrrolino[3,2-c]pyridine core 16 by ortho-lithiation and creation of the biaryl axes via Suzuki cross-coupling reactions. Comparative HPLC studies of racemization for configurationally labile biaryls 31, 38, and 43 containing 1-methyl-2-pyrrolino[3,2-c]pyridine, 4-(dimethylamino)pyridine, and 4-(1-pyrrolidino)pyridine cores, respectively, have demonstrated that a pyrrolidino substituent ortho to the biaryl axis is optimal for slowing Ar-Ar rotation. Biaryls containing all three cores have been shown to retain DMAP-like catalytic activity in the acylation of a hindered alcohol. Biaryls 55 and 56, which are configurationally stable at ambient temperature, have also been prepared via modification of configurationally labile derivatives. Compounds 55 and 56 in optically pure form should provide a useful starting point for studies on catalytic asymmetric acyl transfer using atropisomeric analogues of DMAP.
- Spivey, Alan C.,Fekner, Tomasz,Spey, Sharon E.,Adams, Harry
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p. 9430 - 9443
(2007/10/03)
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- Synthesis of atropisomeric analogues of DMAP
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A method for the preparation of 7-aryl derivatives of N-methyl-5- azaindolinee involving Suzuki cross-coupling is described. Certain biaryls prepared in this manner exhibit atropisomerism. In particular, azaindoline 11 is shown to be configurationally sta
- Spivey, Alan C.,Fekner, Tomasz,Adams, Harry
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p. 8919 - 8922
(2007/10/03)
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