- Desilylation of tert-Butyldimethylsilyl Ethers of Phenols
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Treatment of tert-butyldimethylsilyl ethers of phenols and diphenols with potassium fluoride in the presence of catalytic amounts of hydrobromic acid in dimethylformamide generates the corresponding phenols or diphenols in high yields.
- Sinhababu, Achintya K.,Kawase, Masami,Borchardt, Ronald T.
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Read Online
- Unexpected Regioselectivity in the Lithiation of Fluoroanisoles
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The regioselectivity of lithiation of a series of fluoroanisoles and fluoroveratroles has been studied by determining the ratio of isomeric aldehydes produced by dimethylformamide quenching.The position of lithiation is influenced by such factors as temperature and time of the reaction.Contrary to published reports, fluorine competes significantly with the methoxy group as an ortho director in lithiation reactions.Lithiation of dimethyl-tert-butylsilyl ethers of fluorophenols proceeds exclusively ortho to fluorine.
- Furlano, David C.,Calderon, Silvia N.,Chen, George,Kirk, Kenneth L.
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Read Online
- COMPOUNDS AND COMPOSITIONS FOR USE IN TREATING SKIN DISORDERS
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Provided herein is a compound of formula (XXXII) or a pharmaceutically acceptable salt, solvate, hydrate, stereoisomer thereof or a physiologically functional derivative thereof, wherein R1, R2, R3, G, A, E, n, p, and q are defined herein. Also provided herein are compositions comprising a compound of formula (XXXII), and methods of using a compound of formula (XXXII), e.g., in the treatment or prevention of skin disorders.
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- Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARα Selective Agonist
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BMS-711939 (3) is a potent and selective peroxisome proliferator-activated receptor (PPAR) α agonist, with an EC50 of 4 nM for human PPARα and >1000-fold selectivity vs human PPAR (EC50 = 4.5 μM) and PPAR (EC50 > 100 μM) i
- Shi, Yan,Li, Jun,Kennedy, Lawrence J.,Tao, Shiwei,Hernández, Andrés S.,Lai, Zhi,Chen, Sean,Wong, Henry,Zhu, Juliang,Trehan, Ashok,Lim, Ngiap-Kie,Zhang, Huiping,Chen, Bang-Chi,Locke, Kenneth T.,O'Malley, Kevin M.,Zhang, Litao,Srivastava, Rai Ajit,Miao, Bowman,Meyers, Daniel S.,Monshizadegan, Hossain,Search, Debra,Grimm, Denise,Zhang, Rongan,Harrity, Thomas,Kunselman, Lori K.,Cap, Michael,Muckelbauer, Jodi,Chang, Chiehying,Krystek, Stanley R.,Li, Yi-Xin,Hosagrahara, Vinayak,Zhang, Lisa,Kadiyala, Pathanjali,Xu, Carrie,Blanar, Michael A.,Zahler, Robert,Mukherjee, Ranjan,Cheng, Peter T. W.,Tino, Joseph A.
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supporting information
p. 590 - 594
(2016/07/06)
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- Macrocyclic compounds and methods for their production
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There is provided inter alia compounds of formula (I): for use in treatment of viral infection or as an immunosuppressant.
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Page/Page column 42
(2015/11/10)
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- Sanglifehrin Derivatives and Methods for Their Production
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There are provided inter alia compounds of formula (I) and (II) and their use in therapy, particularly for the treatment of viral infection.
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Paragraph 0163; 0164
(2014/04/03)
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- Novel Dosage Form
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There is provided inter alia a pharmaceutical dosage form for oral administration comprising a sanglifehrin as active ingredient in which the sanglifehrin active ingredient is protected from acid degradation in the stomach environment following oral admin
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Paragraph 0268; 0269
(2014/09/03)
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- NOVEL DOSAGE FORM
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There is provided inter alia apharmaceutical dosage form fororal administration comprising a sanglifehrin as active ingredient in which the sanglifehrin active ingredient is protected from acid degradation in the stomach environment following oral adminis
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Page/Page column 64
(2013/05/21)
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- SUBSTITUTED ACID DERIVATIVES USEFUL AS ANTI-ATHEROSCLEROTIC, ANTI-DYSLIPIDEMIC, ANTI-DIABETIC AND ANTI-OBESITY AGENTS AND METHOD
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Compounds are provided which have the structure of Formula (I): wherein R1 is halogen; and X is hydrogen or halogen, and salts thereof, which compounds are useful as anti-atherosclerotic, anti-dyslipidemic, anti-diabetic, and anti-obesity agent
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Page/Page column 17
(2008/06/13)
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- SUBSTITUTED DIHYDROPYRIDINES AND METHODS OF USE
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Compounds are provided that are modulators of the C5a receptor. The compounds are substituted dihydropyridines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activtation of C5a receptors.
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Page/Page column 126-127
(2010/11/27)
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- NOVEL COMPOUNDS
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Novel inhibitors of Rho-kinases are disclosed.
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Page/Page column 69-70
(2008/06/13)
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- NOVEL AMINOBENZOPHENONE COMPOUNDS
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The invention provides novel compounds according to formula I relates to compounds with the general formula I said compounds being useful, e.g. in the treatment of inflammatory, ophthalmic diseases or cancer.
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- Synthesis of high-specific-radioactivity 4- and 6-[18F]fluorometaraminol- PET tracers for the adrenergic nervous system of the heart
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Fluorine-18 (t12:109.8min)-labeled analogues of metaraminol, 4-[18F]FMR ((1R,2S)-2-amino-1-(4-[18F]fluoro-3-hydroxy phenyl)-1-propanol) and 6-[18F]FMR ((1R,2S)-2-amino-1-(2-[18F]fluoro-5-hydroxyphenyl)-1-propanol), were synthesized as new positron-emission-tomography (PET) tracers for mapping cardiac adrenergic nerve terminals. Copyright
- Langer, Oliver,Dollé, Frédéric,Valette, Héric,Halldin, Christer,Vaufrey, Fran?oise,Fuseau, Chantal,Coulon, Christine,Ottaviani, Michéle,N?gren, Kjell,Bottlaender, Michel,Maziére, Bernard,Crouzel, Christian
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p. 677 - 694
(2007/10/03)
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- tert-BUTYLDIMETHYLSILYL ETHERS OF PHENOLS: THEIR ONE-STEP CONVERSION TO BENZYL OR METHYL ETHERS AND UTILITY IN REGIOSELECTIVE ortho LITHIATION
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A new method for the one-step conversion of tert-butyldimethylsilyl ethers of phenols to benzyl or methyl ethers and the blocking effect of the tert-butyldimethylsilyloxy group in regioselective ortho lithiation are described.
- Sinhababu, Achintya K.,Kawase, Masami,Borchardt, Ronald T.
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p. 4139 - 4142
(2007/10/02)
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- Synthesis and Adrenergic Activity of Ring-Fluorinated Phenylephrines
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2-Fluoro-, 4-fluoro-, and 6-fluorophenylephrine (6-FPE) were synthesized from the corresponding fluorinated 3-hydroxybenzaldehydes.New routes to 2-fluoro- and 6-fluoro-3-hydroxybenzaldehydes were developed based on regioselective lithiation of 2- and 4-fluorobenzene ortho to fluorine.As with norepinephrine and isoproterenol analogues, the adrenergic properties of phenylephrine were markedly altered by ring fluorination.The order of potency of the fluoro analogues as α1-adrenergic agonists in the stimulation of contraction of aorticstrips and of phosphatidylinositol turnover and potentiation of cyclic AMP accumulation in guinea pig synaptoneurosomes was 6-FPE > PE > 4-FPE > 2-FPE.The same pattern was observed for the displacement of radioligands specific for α1- and α2-adrenergic receptors on brain membranes.The order of potency for the displacement of 3H>dihydroalprenolol, a β-specific adrenergic ligand from brain membranes, was 2-FPE > 4-FPE = PE >> 6-FPE. 6-FPE was much more selective for α-adrenergic receptors compared to β-receptors than was phenylephrine.A rationale for the observed fluorine-induced alterations in potency and selectivity of the FPEs for α- and β-adrenergic systems is presented based on fluorine-induced conformations due to electrostatic repulsion of fluorine and the benzyl hydroxyl group.
- Kirk, Kenneth L.,Olubajo, Olarangbe,Buchhold, Konstantin,Lewandowski, Gail A.,Gusovsky, Fabian,et al.
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p. 1982 - 1988
(2007/10/02)
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