- Catalyst-free synthesis of substituted pyridin-2-yl, quinolin-2-yl, and isoquinolin-1-yl carbamates from the corresponding hetaryl ureas and alcohols
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A novel catalyst-free synthesis ofN-pyridin-2-yl,N-quinolin-2-yl, andN-isoquinolin-1-yl carbamates utilizes easily accessibleN-hetaryl ureas and alcohols. The proposed environmentally friendly technique is suitable for the good-to-high yielding synthesis of a wide range ofN-pyridin-2-yl orN-quinolin-2-yl substituted carbamates featuring electron-donating and electron-withdrawing groups in the azine rings and containing various primary, secondary, and even tertiary alkyl substituents at the oxygen atom (48-94%; 31 examples). The DFT calculation and experimental study showed that the reaction proceeds through the intermediate formation of hetaryl isocyanates. The method can be applied to obtainN-isoquinolin-1-yl carbamates, although in lower yields, and ethyl benzo[h]quinolin-2-yl carbamate has also been successfully synthesized (68%).
- Baykov, Sergey V.,Boyarskaya, Irina A.,Boyarskiy, Vadim P.,Geyl, Kirill K.,Kasatkina, Svetlana O.
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p. 6059 - 6065
(2021/07/21)
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- NOVEL COMPOUNDS
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The present invention is directed to novel retinoid-related orphan receptor gamma (RORγ) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORγ.
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Paragraph 0158
(2015/03/16)
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- NOVEL COMPOUNDS
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The present invention is directed to novel retinoid-related orphan receptor gamma (RORγ) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by RORγ.
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Page/Page column 30
(2013/11/18)
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- PIPERIDINE DERIVATIVES USEFUL AS OREXIN ANTAGONISTS
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This invention relates to imidazopyridylmethylene substituted piperidine derivatives orexin antagonists and their use as pharmaceuticals.
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Page/Page column 28
(2010/07/09)
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- Substituted 2-aminopyridines as inhibitors of nitric oxide synthases.
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A series of substituted 2-aminopyridines was prepared and evaluated as inhibitors of human nitric oxide synthases (NOS). 4,6-Disubstitution enhanced both potency and specificity for the inducible NOS with the most potent compound having an IC50 of 28 nM.
- Hagmann,Caldwell,Chen,Durette,Esser,Lanza,Kopka,Guthikonda,Shah,MacCoss,Chabin,Fletcher,Grant,Green,Humes,Kelly,Luell,Meurer,Moore,Pacholok,Pavia,Williams,Wong
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p. 1975 - 1978
(2007/10/03)
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- Metal-Chelating 1,3-bis(2'-Pyridylimino)isoindolines
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A variety of novel chelating 1,3-bis(2'-pyridylimino)isoindoline ligands were prepared and characterized including ligands substituted on both the pyridyl and isoindoline ring systems.Noteworthy are the first isoindoline ligands with solubility in aqueous media.A convenient preparation of 4-alkoxyphthalonitriles is reported; these compounds are readily obtained from 4-nitrophthalonitrile and are suitable starting materials for alkoxy-substituted ligands.
- Siegl, Walter O.
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p. 1613 - 1618
(2007/10/02)
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- 3-TETRAZOLO-5,6,7,8-SUBSTITUTED PYRIDO[1,2-a]PYRIMIDIN-4-ONES
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A novel series of optionally substituted 3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-ones is provided for use as inhibitors of allergic reactions. The compounds exhibit antiallergy activity by both oral and parenteral routes of administration
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