- A bimetallic system for the catalytic hydroxylation of remote primary C- H bonds in functionalized organics using dioxygen
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In a mixture of trifluoroacetic acid and water, the combination of metallic palladium and copper chloride catalyzes the hydroxylation of remote primary C-H bonds of a variety of acids, alcohols, and aliphatic halides, in the presence of carbon monoxide and dioxygen. Experiments suggest that the principal role of metallic palladium is to generate hydrogen peroxide in situ and that the species responsible for the remote hydroxylation of the substrate by hydrogen peroxide is copper chloride. The unusual preference for the catalytic hydroxylation of primary C-H bonds was also found in an experiment involving competition between ethane and either cumene or p- isopropylbenzoic acid: even though the solution concentration of ethane was significantly lower than the competing substrate, the vast majority of the oxidation product (ethanol) was derived from ethane. In the reactions studied, acetic acid and formic acid were formed through C-C cleavage steps. An examination of the site of C-C cleavage in propionic acid indicated that both C-C bonds were being broken.
- Shen, Chengyu,Garcia-Zayas, Eduardo A.,Sen, Ayusman
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- Structure of a novel multidrug resistance modulator, irciniasulfonic acid, isolated from a marine sponge, Ircinia sp.
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Irciniasulfonic acid was obtained from a marine sponge of Ircinia sp. Spectroscopic and chemical analyses revealed its structure consists of three different kinds of acids, i.e. common fatty acids, a novel unsaturated branched C-10 fatty acid and an isethionic acid. Irciniasulfonic acid and deacyl irciniasulfonic acid reverse multidrug resistance in human carcinoma cells caused by overexpression of membrane glycoprotein.
- Kawakami, Ayako,Miyamoto, Tomofumi,Higuchi, Ryuichi,Uchiumi, Takeshi,Kuwano, Michihiko,Van Soest, Rob W. M.
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- CRYSTALLINE SOLID FORMS OF SALTS OF N-{4-[(6,7-DIMETHOXYQUINOLIN-4-YL) OXY]PHENYL}-N'-(4-FLUORPHENYL) CYCLOPROPANE-1,1-DICARBOXAMIDE, PROCESSES FOR MAKING, AND METHODS OF USE
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The invention relates to novel crystalline solid forms of salts of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly renal cell carcinoma (RCC) and medullary thyroid cancer (MTC).
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Paragraph 0372; 0373
(2018/12/13)
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- Process for the production of taurine from ethanol
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The present invention discloses a process for the preparation of taurine from ethionic acid and ethanol by way of ethanol-derived ethionic acid by the ammonolysis of ethionic acid and by the ammonolysis of sodium isethionate and sodium vinyl sulfonate, key intermediates prepared from ethionic acid.
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Page/Page column 6
(2015/09/28)
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- ISETHIONATE SALT OF A SELECTIVE CDK4 INHIBITOR
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Disclosed are polymorphs of the isethionate salt of 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one, which is a selective cyclin-dependent kinase 4 (CDK4) inhibitor useful for treating inflammation and cell proliferative diseases such as cancer and restenosis.
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Page/Page column 24; 25
(2008/06/13)
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- Combinations of signal transduction inhibitors
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The present invention relates to methods for treating cancer comprising utilizing a combination of signal transduction inhibitors. More specifically, the present invention relates to combinations of so called cell cycle inhibitors with mitogen stimulated kinase signal transduction inhibitors, more specifically combinations of CDK inhibitors with mitogen stimulated kinase signal transduction inhibitors, more preferably MEK inhibitors. Other embodiments of the invention relate to additional combinations of the aforesaid combinations with standard anti-cancer agents such as cytotoxic agents, palliatives and antiangiogenics. Most specifically this invention relates to combinations of 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-8H-pyrido[2,3-d]pyrimidin-7-one including salt forms, which is a selective cyclin-dependent kinase 4 (CDK4) inhibitor, in combination with one or more MEK inhibitors, most preferably N-[(R)-2,3-dihydroxy-propoxy]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide. The aforementioned combinations are useful for treating inflammation and cell proliferative diseases such as cancer and restenosis.
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Page/Page column 27
(2010/02/14)
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- PHOTOOXIDATION OF 2-MERCAPTOETHANOL BY VARIOUS WATER-SOLUBLE PHTHALOCYANINES IN AQUEOUS ALKALINE SOLUTION UNDER IRRADIATION WITH VISIBLE LIGHT
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A selection of charged water-soluble phthalocyanines was employed for the photocatalytic oxidation of 2-mercaptoethanol in aqueous alkaline solution in the presence of oppositely charged detergents.Most efficient are Zn(II) and Al(III) phthalocyaninetetrasulfonic acids, which oxidize the thiolate to the sulfonic acid and sulfate, whereas Co(II)phthalocyaninetetrasulfonic acid does not exhibit a photoeffect.During the photooxidation reactions, decomposition (photobleaching) of the zinc phthalocyanine derivatives occurs, whereas the analogues alumina chelates are more stable.Covalent binding of Zn(II)phthalocyanine derivatives to silica carriers resulted in photocatalytic activities even in the absence of detergents, since the immobilization of the complexes preserves the required monomeric state, Moreover, the photodecomposition (bleaching) of the heterogenized complexes is strongly retarded.For the photooxidations mainly the pathway via the sensitized formation of singlet oxygen with subsequent oxidation reactions is valid.Hydrogen peroxide as one reduction product of oxygen was found.
- Schneider, Gerhard,Woehrle, Dieter,Spiller, Wolfgang,Stark, Johannes,Ekloff-Schulz, Guenther
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p. 333 - 342
(2007/10/02)
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