- Syntheses of 4-(Heteroaryl)cyclohexanones via Palladium-Catalyzed Ester α-Arylation and Decarboxylation
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An alternative synthesis of 4-(heteroaryl)cyclohexanones is described featuring a palladium-catalyzed ester α-arylation followed by decarboxylation. The substrate scope is broad with a wide range of heteroaryl halides. In particular, the reaction robustness is demonstrated by the synthesis of >10 g of 4-(pyrazin-2-yl)cyclohexanone with 85% overall yield.
- Zhou, Jianguang,Jiang, Qun,Fu, Peng,Liu, Siqian,Zhang, Sisi,Xu, Su,Zhang, Qi
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p. 9851 - 9858
(2017/09/23)
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- Remote Oxidation of Aliphatic C-H Bonds in Nitrogen-Containing Molecules
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Nitrogen heterocycles are ubiquitous in natural products and pharmaceuticals. Herein, we disclose a nitrogen complexation strategy that employs a strong Bronsted acid (HBF4) or an azaphilic Lewis acid (BF3) to enable remote, non-directed C(sp3)-H oxidations of tertiary, secondary, and primary amine- and pyridine-containing molecules with tunable iron catalysts. Imides resist oxidation and promote remote functionalization.
- Howell, Jennifer M.,Feng, Kaibo,Clark, Joseph R.,Trzepkowski, Louis J.,White, M. Christina
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p. 14590 - 14593
(2015/12/08)
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- CYCLOHEXYL-AZETIDINYL ANTAGONISTS OF CCR2
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The present invention comprises compounds of Formula (I). Wherein: R1, R2, R4, J, Q, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
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Page/Page column 139
(2012/01/06)
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- 7-CYCLOALKYLAMINOQUINOLONES AS GSK-3 INHIBITORS
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Provided herein are aminoquinolones of formula I and compositions containing the compounds. The compounds and compositions provided herein are useful in the prevention, amelioration or treatment of GSK-3 inhibitors mediated diseases.
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Page/Page column 25
(2010/09/18)
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- Benzamide derivatives and uses related thereto
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Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.
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Page/Page column 59-60
(2008/06/13)
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- Cardiotonic Agents. 1-Methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3(2H)-isoquinolinones and Related Compounds. Synthesis and Activity
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A series of 1-methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3(2H)-isoquinolinones and related compounds were synthesized and evaluated for positive inotropic activity.Most members of this series exerted a dose-dependent increase in myocardial contractility in the dog acute heart failure model, whereas they caused only slight changes in heart rate and blood pressure.Several derivatives, especially those with cyano, acetyl, and ethyl substituents at the 4-position, were more potent than milrinone, which was used as a reference. 4-Acetyl-1-methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3(2H)-isoquinolinone (MS-857) is one of the most potent positive inotropic agents in this series.
- Kaiho, Tatsuo,San-nohe, Kunio,Kajiya, Seitaro,Suzuki, Tsuneji,Otsuka, Kengo,et al.
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p. 351 - 357
(2007/10/02)
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- Isoquinoline derivative
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An isoquinoline derivative of the following formula: STR1 wherein R1 is a methyl or a methoxymethyl group and R2 and R3 are each a hydrogen atom or a methyl, ethyl, methoxy, a cyclohexyl, a phenyl, a 3,4-dimethoxyphenyl, a
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