- Pd-Catalyzed Decarboxylative Ortho-Halogenation of Aryl Carboxylic Acids with Sodium Halide NaX Using Carboxyl as a Traceless Directing Group
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A highly regioselective Pd-catalyzed carboxyl directed decarboxylative ortho-C-H halogenation of cheap o-nitrobenzoic acids with NaX (X = I, Br) under aerobic conditions has been established. The utility of the method has been demonstrated by the gram-scale reaction and derivatization of the product. Experimental results have confirmed Pd and Bi played critical roles in the transformation and indicated the transformation might proceed via 2-halo-6-nitrobenzoic acid derivative intermediate.
- Fu, Zhengjiang,Jiang, Yongqing,Wang, Shuiliang,Song, Yuanyuan,Guo, Shengmei,Cai, Hu
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supporting information
p. 3003 - 3007
(2019/05/10)
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- Kynurenic acid derivatives useful in the treatment of neurodegenerative disorders
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4-Oxo-1,4-dihydroquinoline compounds having a 2-acidic group or a group convertible thereto in vivo, and their pharmaceutically acceptable salts, are potent specific antagonists of N-methyl-D-aspartate (NMDA) receptors and are therefore useful in the treatment of neurodegenerative disorders. 4-Oxo-1,4-dihydroquinoline compounds having a 2-acidic group or a group convertible thereto in vivo, other than carboxy or C 1-6 alkoxycarbonyl, are novel compounds, as also are compounds of formula II STR1 wherein R 2 represents carboxy or a group convertible thereto in vivo, R 6 is hydrogen and R 5 and R 7 represent C 1-6 alkyl or halogen, provided that R 5 and R 7 are not simultaneously chlorine or simultaneously bromine; a process for preparing the novel compounds is described, as also are pharmaceutical compositions containing the novel compounds.
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- Kynurenic Acid Derivatives. Structure-Activity Relationships for Excitatory Amino Acid Antagonism and Identification of Potent and Selective Antagonists at the Glycine Site of the N-Methyl-D-aspartate Receptor
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Derivatives of the nonselective excitatory amino acid antagonist kynurenic acid (4-oxo-1,4-dihydroquinoline-2-carboxylic acid, 1) have been synthesized and evaluated for in vitro antagonist activity at the excitatory amino acid receptors sensitive to N-me
- Leeson, Paul D.,Baker, Raymond,Carling, Robert W.,Curtis, Neil R.,Moore, Kevin W.,et al.
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p. 1243 - 1252
(2007/10/02)
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