- 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 42-43
(2012/07/27)
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- Synthetic Routes to the Carcinogen IQ and Related 3H-Imidazoquinolines
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2-Amino-3-methyl-3H-imidazoquinoline (IQ, 1a) and four new IQ homologues, viz. its 7-methyl, 8-methyl, 9-methyl and 7,9-dimethyl derivatives 1c-1f, have been conveniently synthesized from the appropriate 6-methoxyquinolines 3 rather than from the p
- Ronne, Erik,Grivas, Spiros,Olsson, Kjell
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p. 823 - 830
(2007/10/02)
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- Oxidative Methylamination of Nitroquinolines
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3-, 5-, 6-, 7- and 8-nitroquinoline as well as 5,7- and 6,8-dinitroquinoline are methylaminated with a liquid methylamine solution of potassium permanganate (LMA/PP) to the corresponding mono- and bis(methylamino)-substituted compounds. 2-Nitroquinoline is aminated with LMA/PP to 2-(methylamino)quinoline.The intermediate methylamino ?-adducts of 3-nitro- and 5,7- and 6,8-dinitroquinoline are detected by 1H-NMR spectroscopy.Quantum chemical calculations for the mononitroquinolines suggest that the experimentally observed regioselectivity of the methylamination is controlled by an interaction of frontal molecular orbitals (FMO) of the reagents. Key Words: Methylaminations / ?-Adducts, methylamino / Calculations, FMO / Quinolines / Aminations
- Wozniak, Marian,Grzegozek, Maria
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p. 823 - 830
(2007/10/02)
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- BIOLOGICAL FORMATION AND CHEMICAL SYNTHESIS OF 2-AMINO-3,6-DIHYDRO-3-METHYL-7H-IMIDAZOLOQUINOLIN-7-ONE, THE MAJOR METABOLITE OF THE DIETARY CARCINOGEN 2-AMINO-3-METHYL-3H-IMIDAZOLOQUINOLINE (IQ) BY NORMAL INTESTINAL BACTERIA
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2-Amino-3,6-dihydro-3-methyl-7H-imidazoloquinolin-7-one (2) has been synthesized from 6-bromo-5-nitroquinoline in seven steps.Biological formation of 2 from IQ (1) involves the addition of water from the medium, followed by oxidation.
- Bashir, Mohammad,Kingston, David G. I.,Carman, Robert J.,Tassell, Roger L. van,Wilkins, Tracy D.
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p. 2877 - 2886
(2007/10/02)
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