- ANTIVIRAL COMPOUNDS
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The present invention relates to novel compounds of general formula (I) wherein the groups X, and R1 to R4 have the meanings given in the description and claims, process for preparing these compounds and their use as for treating, preventing or ameliorating viral infections and their use for treating, preventing or ameliorating diseases which are associated with PLA2G16.
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Paragraph 0587
(2018/04/13)
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- Manganese catalyzed cis-dihydroxylation of electron deficient alkenes with H2O2
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A practical method for the multigram scale selective cis-dihydroxylation of electron deficient alkenes such as diethyl fumarate and N-alkyl and N-aryl-maleimides using H2O2 is described. High turnovers (>1000) can be achieved with this efficient manganese based catalyst system, prepared in situ from a manganese salt, pyridine-2-carboxylic acid, a ketone and a base, under ambient conditions. Under optimized conditions, for diethyl fumarate at least 1000 turnovers could be achieved with only 1.5 equiv. of H2O2 with d/l-diethyl tartrate (cis-diol product) as the sole product. For electron rich alkenes, such as cis-cyclooctene, this catalyst provides for efficient epoxidation.
- Saisaha, Pattama,Pijper, Dirk,Van Summeren, Ruben P.,Hoen, Rob,Smit, Christian,De Boer, Johannes W.,Hage, Ronald,Alsters, Paul L.,Feringa, Ben L.,Browne, Wesley R.
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supporting information; experimental part
p. 4444 - 4450
(2010/11/05)
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- Covalent heterogenization of a discrete Mn(II) Bis-Phen complex by a metal-template/metal-exchange method: An epoxidation catalyst with enhanced reactivity
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Considerable attention has been devoted to the immobilization of discrete epoxidation catalysts onto solid supports due to the possible benefits of site isolation such as increased catalyst stability, catalyst recycling, and product separation. A synthetic metal-template/metal-exchange method to imprint a covalently attached bis-1,10-phenanthroline coordination environment onto high-surface area, mesoporous SBA-15 silica is reported herein along with the epoxidation reactivity once reloaded with manganese. Comparisons of this imprinted material with material synthesized by random grafting of the ligand show that the template method creates more reproducible, solution-like bis-1,10-phenanthroline coordination at a variety of ligand loadings. Olefin epoxidation with peracetic acid shows the imprinted manganese catalysts have improved product selectivity for epoxides, greater substrate scope, more efficient use of oxidant, and higher reactivity than their homogeneous or grafted analogues independent of ligand loading. The randomly grafted manganese catalysts, however, show reactivity that varies with ligand loading while the homogeneous analogue degrades trisubstituted olefins and produces trans-epoxide products from cis-olefins. Efficient recycling behavior of the templated catalysts is also possible.
- Terry, Tracy J.,Daniel,Stack
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p. 4945 - 4953
(2008/09/21)
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- The synthesis of solvent-free glycidic esters from diazoesters and carbonyl compounds catalysed by lanthanide trifiates
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The results of the reaction between ethyl diazoacetate and carbonyl compounds catalysed by lanthanide triflates are described. Aldehydes, and α-unsubstituted and α-monosubstituted cyclohexanones react to give the selective formation of α,β-epoxy esters (g
- Curini, Massimo,Epifano, Francesco,Marcotullio, Maria Carla,Rosati, Ornelio
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p. 1562 - 1565
(2007/10/03)
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- Practical synthesis of optically pure methyl (2R,3S)-2,3-epoxybutanoate via microbial asymmetric reduction of α-chloroacetoacetate
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Asymmetric reduction of ethyl α-chloroacetoacetate (3) with Baker's yeast followed by treatment with sodium ethoxide afforded a mixture of ethyl (2R,3S)-(8) and (2S,3S)-2,3-epoxybutanoate (9) (8/9, 85:15), which could be converted into the optically pure methyl (2R,3S)-2,3-epoxybutanoate (25) via one recrystallization of the brucine salt of the diastereomeric mixture of the corresponding epoxy acid.
- Akita,Todoroki,Endo,Ikari,Oishi
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p. 513 - 516
(2007/10/02)
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- Synthesis and Reactions of 3-Hydroxy-2-nosyloxy Esters Produced by the Stereoselective Reduction of 2-Nosyloxy-3-keto Esters
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The reduction of 2-nosyloxy-3-keto esters is an effective method for the preparation of 3-hydroxy-2-nosyloxy esters.The reduction is stereoselective for the syn isomer.The anti isomer can be produced as the major product by the addition of p-nitrobenzenesulfonyl peroxide to ketene bis-silyl acetal derivatives of 3-hydroxy esters.The diastereomers are separable chromatographically and can be converted stereospecifically to glycidic esters and 2-azido-3-hydroxy esters.As such they appear to have excellent potential as versatile synthetic intermediates for the synthesis of 1,2,3-trifunctional substances.
- Hoffman, Robert V.,Kim, Hwa-Ok
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p. 6759 - 6764
(2007/10/02)
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- Regioselective AlPO4-Al2O3 Promoted Ring-Opening of 2,3-Epoxy Esters
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Synthesic AlPO4-Al2O3 promotes regioselective ring-opening of 2,3-epoxy esters by some oxygen and sulphur nucleophiles.Ritter type ring-opening with acetonitrile allowed the regioselective introduction of the acetamido group.
- Riego, Juan,Costa, Antonio,Saa, Jose Manuel
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p. 1565 - 1568
(2007/10/02)
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