- Desymmetrizing Isomerization of Alkene via Thiazolinyl Iminoquinoline Cobalt Catalysis
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We report a cobalt-catalyzed desymmetrizing isomerization of exo-cyclic alkenes to generate chiral 1-methylcyclohexene derivatives with good yields and enantioselectivities. A novel chiral thiazolinyl iminoquinoline ligand and its cobalt complex were desi
- Liu, Wenbo,Zheng, Yushan,Mao, Yihui,Chen, Jieping,Ren, Xiang,Cheng, Zhaoyang,Lu, Zhan
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supporting information
p. 1158 - 1163
(2022/02/14)
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- Visible Light Mediated Generation of trans-Arylcyclohexenes and Their Utilization in the Synthesis of Cyclic Bridged Ethers
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While accessible via UV-irradiation of cis-cyclohexene, trans-cyclohexene has thus far been an investigation driven by curiosity, and due primarily to its short lifespan, has until recently not been employed for productive synthesis. Herein, we present st
- Day, Jon I.,Singh, Kamaljeet,Trinh, Winston,Weaver, Jimmie D.
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supporting information
p. 9934 - 9941
(2018/07/25)
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- 4-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2
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The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 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 50
(2010/11/03)
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- Incorporation of 2-arylhexa-1,5-diene into pentasil zeolite: A distorted 1-arylcyclohexane-l,4-diyl radical cation at room temperature
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Incorporation into a redox-active pentasil zeolite [(Na,H)-ZSM-5] converted 2-arylhexa-1,5-dienes (9a-c; aryl = phenyl, tolyl, anisyl) into 1-arylcyclohexane-1,4-diyl radical cations, 10a-cì?+. The ESR spectra of 10a-cì?+ (six lines,
- Ikeda, Hiroshi,Minegishi, Tomonori,Miyashi, Tsutomu,Lakkaraju, Prasad S.,Sauers, Ronald R.,Roth, Heinz D.
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p. 2504 - 2511
(2007/10/03)
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- Triphenylpyrylium salt-sensitized photoreactions of 1,4-diaryl-2,3- dioxabicyclo[2.2.2]octanes through competitive single electron-transfer pathway and proton-catalyzed pathway
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2,4,6-Triphenylpyrylium tetrafluoroborate (TPPBF4)-sensitized photoinduced electron-transfer (PET) reactions of 1,4-diaryl-2,3-dioxabicyclo[2. 2.2]octanes 5 (a: Ar1 = Ar2 = p-MeOC6H 4, b: Ar1 = Ar2 = p-MeC6H 4, c: Ar1 = Ar2 = Ph) underwent novel fragmentation through their radical cations to give 1,4-diarylbutan-1,4-diones 6 accompanied by elimination of ethylene. On the other hand, 4-aryl-cyclohex-3- en-1-ones 7, p-substituted phenols 8, and 4-aryl-4-aryloxycyclohexanones 9 were produced through proton-catalyzed pathways when the PET reactions of 5 were performed in the absence of a certain base such as 2,6-di-tert-butylpyridine (DTBP). Particularly, the formation of 9 is consistent with the novel cationic rearrangement involving nucleophilic O-1,2-aryl shifts and C-1,4-aryl shifts.
- Kamata, Masaki,Kaneko, Jun-Ichi,Hagiwara, Jun-Ichi,Akaba, Ryoichi
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p. 7423 - 7428
(2007/10/03)
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- Synthesis and biological evaluation of cycloalkylidene carboxylic acids as novel effectors of Ras/Raf interaction
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The protooncogenes Ras and Raf play important roles in signal transduction pathways regulated by mitogen-activated protein kinases. Mutations of Ras that arrest the protein in its active state are frequently implicated in tumor formation. We used Ras and Raf proteins in the yeast two-hybrid system to search for natural or synthesized substances capable of modulating Ras/Raf interaction by specifically binding to one of the interacting partners. We found that cycloalkylidene carboxylic acids enhanced Ras/Raf interaction by acting on the cysteine-rich domain of Raf. Several analogues of the active substance 2-cyclohexylidene propanoic acid were synthesized and the importance of the semicyclic double bond in the stabilization of Ras/Raf interaction was demonstrated. Variation of the size and the substituents of the cyclic system as well as the length of the carboxylic acid resulted in enhanced Ras/Raf interaction.
- Friese, Anke,Hell-Momeni, Katja,Zündorf, Ilse,Winckler, Thomas,Dingermann, Theodor,Dannhardt, Gerd
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p. 1535 - 1542
(2007/10/03)
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- Fe(II)-mediated fragmentation of 1,4-diaryl-2,3-dioxabicyclo[2.2.2]octanes through competitive single electron transfer pathway and Lewis acid pathway
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Reactions of 1,4-diaryl-2,3-dioxabicyclo[2.2.2]octanes 1a-d (1a: Ar=p-FC6H4, 1b: Ar=Ph, 1c: Ar=p-MeC6H4, 1d: Ar=p-MeOC6H4) with FeBr2 in THF afforded 1,4-diarylbutan-1,4-diones 2a-d and 1,4-diaryl-7-oxabicyclo[2.2.1]heptanes 3a-d. On the other hand, 4-aryl-3-cyclohexenones 4c-d and p-substituted phenols 5c-d were obtained in the reactions of 1c-d with FeBr2 in CH2Cl2. A new fragmentation mechanism involving an electrophilic oxyl radical 1,5-substitution and a nucleophilic O-1,2-aryl shift is proposed based on the product analysis. In addition, the in vitro antimalarial activities of 1a-d were tested.
- Kamata, Masaki,Kudoh, Takashi,Kaneko, Jun-Ichi,Kim, Hye-Sook,Wataya, Yusuke
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p. 617 - 620
(2007/10/03)
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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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