- PYRIDINE CARBOXALDEHYDE-BASED SYNTHESIS OF OXYGEN-CONTAINING HETEROCYCLES
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Heterocycles containing one or two atoms of oxygen are synthesized by the condensation of pyridine carboxaldehydes with ethylene glycol, 1,3-propanediol, and 3-methyl-3-buten-1-ol.When the unsaturated alcohol is used, linear acetal are formed along with the cyclic products.
- Ibatullin, U. G.,Petrushina, T. F.,Leitis, L. Ya.,Plesanova, I.N.,Skolmeistere, R. A.,et al.
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- Uncommon reaction of 2-bromomethyl-1,3-thiaselenole with pyridine and its derivatives
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Regioselective reaction of 2-bromomethyl-1,3-thiaselenole with pyridine and its derivatives is followed by rearrangement with ring expansion and the formation of a bond between a nitrogen atom and a carbon in the position 2. A set of derivatives of 2,3-dihydro-1,4-thiaselenine was obtained, substituted in the position 2 by a pyridinium residue functionalized by pharmacophoric groups.
- Amosova,Penzik,Rykunova, Yu. I.,Potapov,Albanov
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- COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES
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The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound useful in the treatment of a neurodegenerative disorder and their combined use as a medicament, in particular for the treatment of neurodegenerative and/or cognitive disorders.
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Page/Page column 116
(2019/07/19)
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- 1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS
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The present invention provides 1H-pyrazolo[4,3-b]pyridines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
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Paragraph 0548-0549
(2019/07/10)
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- COMBINATION TREATMENTS COMPRISING ADMINISTRATION OF 1H-PYRAZOLO[4,3-B]PYRIDINES
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The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors together with a second compound which compound is useful in the treatment of a psychiatric disorder and their combined use as a medicament, in particular for the treatment of psychiatric and/or cognitive disorders.
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Page/Page column 113
(2019/07/19)
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- 1H-PYRAZOLO[4,3-B]PYRIDINES AS PDE1 INHIBITORS
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The present invention provides 1H-pyrazolo[4,3-b]pyridin-7-amines of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.
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Page/Page column 107
(2018/09/25)
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- NaBH4-TMEDA and a palladium catalyst as efficient regio- and chemoselective system for the hydrodehalogenation of halogenated heterocycles
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The pair NaBH4-TMEDA as hydride source and a palladium catalyst in THF prove to be an efficient system for the hydrodehalogenation of halogenated heterocycles with one or more heteroatoms. In general, Pd(OAc) 2-PPh3 rapidly hydrodehalogenates reactive halo-heterocycles such as bromo-pyridines, -quinolines, -thiophenes, -indoles, -imidazoles, etc., at room temperature in very good yields, whereas in most cases PdCl2(dppf) reduces less reactive halides such as chloro-pyridines, -quinolines, -pyrimidines and bromo-indoles, -benzofurans, etc. Moreover, PdCl2(tbpf) shows to be even more active removing the 2- and 5-chlorine from both thiophene and thiazole rings. The reaction conditions tolerate various functional groups, allowing highly chemoselective reactions in the presence of halide, ester, alkyne, alkene and nitrile substituents. Moreover, with a proper selection of the catalyst it is also possible to obtain a good control in the regioselective hydrodehalogenation of a variety of polyhalogenated substrates.
- Chelucci, Giorgio,Figus, Susanna
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p. 191 - 209
(2014/07/21)
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- Hydrodehalogenation of halogenated pyridines and quinolines by sodium borohydride/N,N,N′,N′-tetramethylethylenediamine under palladium catalysis
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A protocol for the hydrodehalogenation of halogenated pyridines and quinolines by the sodium borohydride/N,N,N′,N′-tetramethylethylenediamine (NaBH4-TMEDA) system under palladium catalysts is reported. Catalytic amounts of [1,1′-bis(diphenylphosphino)ferrocene] dichloropalladium(II) in combination with NaBH4-TMEDA rapidly hydrodehalogenate chloro(bromo)-pyridines and -quinolines at room temperature in quantitative yields. Chemoselective reduction of 4,7-dichloroquinoline affords 7-chloroquinoline as the sole product in almost quantitative yield. Moreover, palladium(II) acetate-triphenylphosphine and NaBH4-TMEDA are able to reduce efficiently reactive bromo-pyridines and -quinolines.
- Chelucci, Giorgio
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experimental part
p. 1562 - 1565
(2010/06/14)
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- Reduction of n-(1,3-Dioxolan-2-yl)-1-methylpyridinium Ions: Molecular Structure of the 4-(1,3-Dioxolan-2-yl)-1-methyl-1,2,3,6-tetrahydropyridine-Borane Complex
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The reduction of the n-(1,3-dioxolan-2-yl)-1-methylpyridinium ions with sodium borohydride has been studied to prepare N-methylformylpiperidines.Deuterium oxide was used as the solvent in order to assign the protons in the nmr spectra.As a product of the reaction, the 4-(1,3-dioxolan-2-yl)-1-methyl-1,2,3,6-tetrahydropyridine-borane complex, was isolated and crystallized.A X-ray study of this borane complex has been carried out.
- Rodriguez, J. G.,Martinez-Lopez, N.,Lerma, J. Lopez de,Perales, A.
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p. 135 - 139
(2007/10/02)
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- Synthesis of 1'-Methylspiro from 1-Methyl-n-piperidinecarbaldehydes
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1'-Methylspiro 2 can be obtained from 1-methyl-n-piperidinecarbaldehydes 1 by the Fischer reaction of their phenylhydrazones.The Fischer reaction provides different kinds of products -3H-indole, indole and oxindole- which depend on the N atom position in the piperidine ring.
- Benito, Y.,Canoira, L.,Martinez-Lopez, N.,Rodriguez, J. G.,Temprano, F.
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p. 623 - 628
(2007/10/02)
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- 13C NMR SPECTRAL AND STEREOCHEMICAL ANALYSIS OF PIPERIDINE DERIVED α-AMINONITRILES
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Carbon-13 NMR spectra of several α-aminonitriles are reported, along with their preparation via the modified Polonovski reaction or the reductive cyanation of Fry.The substituent effects for the cyano group in the different nitrogen heterocycles were dete
- Jokela, Reija,Tamminen, Tarja,Lounasmaa, Mauri
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p. 1707 - 1722
(2007/10/02)
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