- Favorski type rearrangement in the lead tetraacetate oxidation of cycloalkanones
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The cycloalkanones (1a-1f) have been converted into their corresponding cycloalkane carboxylates (2a-2f) by a lead(IV) acetate promoted rearrangement in presence of perchloric acid in triethyl orthoformate.
- Mathew, Felix,Myrboh, Bekington
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Read Online
- Synthesis of 3-hydroxyindanones via potassium salt of amino acid catalyzed regioselective intramolecular aldolization of ortho-diacylbenzenes
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First organocatalytic intramolecular aldolization of ortho-diacylbenzenes to construct highly functionalized 3-hydroxyindanones is described. In this transformation a high trans-selectivity is achieved by the use of metal salt of amino acid. This method allows an easy access to the strained spirocyclic 3-hydroxyindanones related to a number of natural product frameworks. Synthesis of a new class of indole skeleton substituted by 3-hydroxyindanones added an extra essence to this new protocol.
- Chanda, Tanmoy,Chowdhury, Sushobhan,Anand, Namrata,Koley, Suvajit,Gupta, Ashutosh,Singh, Maya Shankar
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supporting information
p. 981 - 985
(2015/03/04)
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- METHOD OF TREATMENT
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The present invention relates to a method of treating T cell mediated inflammatory immune diseases or T cell mediated hypersensitivity diseases, which comprises administering to a human in need thereof an effective amount of a compound which inhibits EZH2 and/or EZH1, or a pharmaceutically acceptable salt thereof.
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Paragraph 0771
(2014/09/29)
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- ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
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This invention relates to novel substituted benzamide according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
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Page/Page column 56
(2013/12/03)
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- General Synthesis of Methyl- and Dimethyl-cyclobutanes from Simple 1,3-Diols by Phase Transfer Catalysis
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A general method is described for the preparation of methyl- and dimethyl-cyclobutanes from simple 1,3-diols.The key steps of the procedure are a phase transfer catalysed ring closure and the transformation of a carboxyl group to a methyl group.Phase transfer catalysis provides good yields in the synthesis of the cyclobutane skeleton.
- Toeroek, Bela,Molnar, Arpad
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p. 801 - 804
(2007/10/02)
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- Direct Observation of α-Oxo Ketenes from the Photolysis of α-Diazo β-Diketones
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Monitoring by IR spectroscopy of the broad-band irradiation of the symmetrically substituted 2-diazocyclohexane-1,3-dione (11), 3-diazopentane-2,4-dione (19), and 4-diazo-2,2,6,6-tetramethylheptane-3,5-dione (24) in Ar matrices at 12 K showed the formation of 2-carbonylcyclopentanone (s-Z-12), acetyl(methyl)ketene (s-E-20), and tert-butyl(pivaloyl)ketene (s-E-25), respectively, in less than 10 min.On increasing the photolysis time to >3 h, the α-oxo ketenes 12, 20, and 25 decarbonylated to the corresponding oxocarbenes which underwent Wolff rearrangement to carbonylcyclobutane (15), dimethylketene (23), and di-tert-butylketene (28), respectively.The reaction of 2-carbonylcyclopentanone (12) with CH3OH was monitored by IR spectroscopy.Thus, it was found that the reaction started at ca. 100 K and was essentially complete at 140 K, involving the initial formation of the enol form (9) of methyl 2-oxocyclopentanecarboxylate.
- Leung-Toung, Regis,Wentrup, Curt
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p. 4850 - 4858
(2007/10/02)
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- Hydrogenolysis of Small Cycloalkanes, XI. - Hydrogenation of Bicyclobutane-1- and -2-carboxylates
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Hydrogenation of ethyl bicyclobutane-2-carboxylate (1) with Pd/C in ethanol at normal conditions leads to 95 percent of ethyl 2-methylbutyrate (2) and 5 percent of ethyl n-valerate (3).The corresponding 1-carboxylic acid ester 8 yields 99 percent of 2 but less than 1 percent of cyclobutane as well as the cis- and trans-2-methylcyclopropanecarboxylates 5 and 9.In this case 2-methylenebutyric and cis- and trans-2-methylcrotonic acid esters (10, 11a, and 12) can be detected as intermediates.From these, conclusions can be made about the mechanism at the catalyst. 5 is the main product with a poisoned catalyst.
- Hertzsch, Winfried,Musso, Hans
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p. 1485 - 1491
(2007/10/02)
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- Crown ether catalysis of decarboxylation and decarbalkoxylation of β-keto acids and malonates: a synthetic application
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The effect of 18-crown-6 ether on the decarboxylation rates of the sodium and potassium salts of 3-camphor carboxylic acid 1 and of 1-carbomethoxy-1-carboxycyclohexane 2 was studied.For 2 the K-18C6 salt reacted ca. 104 times faster than the parent acid.This remarkable difference in reactivity was used in developing a one-pot, two-step procedure for decarbalkoxylation of malonic esters.This procedure was then applied to a range of malonates, β-keto esters, and an α-cyano ester.The effect of 15C5, other cations, and good nucleophiles was also studied.
- Hunter, Duncan H.,Patel, Vijay,Perry, Richard A.
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p. 2271 - 2277
(2007/10/02)
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