- HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
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Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.
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Page/Page column 47
(2012/07/27)
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- HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF
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Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes
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Page/Page column 133
(2011/12/14)
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- Amination and Synthesis of Some Nitronaphthyridines
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3-Nitro and 3,6-dinitro-1,8-naphthyridines 1, 4 and 5 are dehydroaminated with a liquid ammonia solution of potassium permanganate to the corresponding 4-amino-substituted compounds 3, 8 and 9.The intermediate 4-amino ?-adducts 2,6 and 7 of the nitro-1,8-naphthyridines are detected by 1H-NMR spectroscopy.The syntheses of some nitro-substituted naphthyridines are described. Key Words: Amination / Amino ?-adducts / Naphthyridines
- Wozniak, Marian,Tomula, Maria
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p. 471 - 476
(2007/10/02)
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- Chichibabin Amination of 1,X-Naphthyridines. Nuclear Magnetic Resonance Studies on the ? Adducts of Heterocyclic Systems with Nucleophiles
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In the amination of 1,X-naphthyridines with potassium amide in liquid ammonia at about -35 to -40 deg C the initial adduct formation is charge controlled.Thus, at these temperatures the site with the lowest electron density is most susceptible for amide attack (C-2 in 1,5-naphthyridine, C-2 in 1,6-naphthyridine, C-2 and C-8 in 1,7-naphthyridine, and C-2 in 1,8-naphthyridine), as proven by NMR spectroscopy.When the temperature was raised to about 10 deg C, the site of addition has been found to change for 1,5- and 1,7-naphthyridine (NMR spectroscopy): from C-2 to C-4 in 1,5-naphthyridine and from C-2 and C-8 to C-8 only in 1,7-naphthyridine.In case of 1,6- and 1,8-naphthyridines no change was observed.Thus, the amination at about 10 deg C is a process which is thermodynamically controlled.The several factors which contribute to the stability of these addition products have been discussed.It has been found that the anionic ? adducts 2(4,8)-aminodihydro-1,X-naphthyridinides can be easily oxidized with potassium permanganate into their corresponding 2(4,8)-amino-1,X-naphthyridines.
- Haak, Henk J. W. van den,Plas, Henk C. van der,Veldhuizen, Beb van
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p. 2134 - 2137
(2007/10/02)
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