- Nucleophilic Organic Base DABCO-Mediated Chemospecific Meinwald Rearrangement of Terminal Epoxides into Methyl Ketones
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Nucleophilic organic base DABCO (1,4-diazabicyclo[2.2.2]octane)-mediated Meinwald rearrangement of various epoxides was investigated. 2-Aryl-, alkenyl-, and alkynylepoxides generate the corresponding methyl ketones chemospecifically in good to excellent yields. The current DABCO-mediated Meinwald rearrangement of epoxides features readily accessible starting materials, a wide substrate scope, a transition-metal- and acid-free environment, and chemospecificity in the isomerization of epoxides.
- Li, Siqi,Shi, Yi,Li, Pingfan,Xu, Jiaxi
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p. 4443 - 4450
(2019/04/30)
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- Manganese(II)/Picolinic Acid Catalyst System for Epoxidation of Olefins
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An in situ generated catalyst system based on Mn(CF3SO3)2, picolinic acid, and peracetic acid converts an extensive scope of olefins to their epoxides at 0 °C in 5 min, with remarkable oxidant efficiency and no evidence of radical behavior. Competition experiments indicate an electrophilic active oxidant, proposed to be a high-valent Mn = O species. Ligand exploration suggests a general ligand sphere motif contributes to effective oxidation. The method is underscored by its simplicity and use of inexpensive reagents to quickly access high value-added products.
- Moretti, Ross A.,Du Bois,Stack, T. Daniel P.
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supporting information
p. 2528 - 2531
(2016/07/06)
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- Novel Ethanediamone Hepcidine Antagonists
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The present invention relates to novel hepcidin antagonists of formula (I), pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for treatment of disorders in iron metabolism, such as, in particular, iron deficiency diseases and anaemias, in particular anaemias in connection with chronic inflammatory diseases (ACD: anaemia of chronic disease and AI: anaemia of inflammation).
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- HETEROCYCLIC COMPOUNDS
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The invention is related to novel substituted diazaheterocycles useful as effective antihypercholesterolemic agents, methods of their preparation, and pharmaceutical compositions containing them.
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Page/Page column 19
(2008/06/13)
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- Oxazolidinones as novel human CCR8 antagonists
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High-throughput screening of the corporate compound collection led to the discovery of a novel series of N-substituted-5-aryl-oxazolidinones as potent human CCR8 antagonists. The synthesis, structure-activity relationships, and optimization of the series
- Jin, Jian,Wang, Yonghui,Wang, Feng,Kerns, Jeffery K.,Vinader, Victoria M.,Hancock, Ashley P.,Lindon, Matthew J.,Stevenson, Graeme I.,Morrow, Dwight M.,Rao, Parvathi,Nguyen, Cuc,Barrett, Victoria J.,Browning, Chris,Hartmann, Guido,Andrew, David P.,Sarau, Henry M.,Foley, James J.,Jurewicz, Anthony J.,Fornwald, James A.,Harker, Andy J.,Moore, Michael L.,Rivero, Ralph A.,Belmonte, Kristen E.,Connor, Helen E.
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p. 1722 - 1725
(2007/10/03)
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- INHIBITORS OF AKT ACTIVITY
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Invented are novel 1 H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 125
(2008/06/13)
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- NOVEL DERIVATIVES OF PYRIDYLETHANOL (PHENYLETHYL) AMINES AS INHIBITORS OF CHOLESTEROL BIOSYNTHESIS, PROCESSES FOR THEIR PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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The novel derivatives of pyridylethanol (phenylethyl) amines of formula I are described wherein n is an integer from 1 to 4, R1 is a hydrogen atom, hydroxyl group or lower C1-6 alkoxy group R2 is a hydrogen atom or a straight or branched lower C1-6 alkyl group X, is hydrogen, fluorine, chlorine, bromine, hydroxyl group, trifluoromethyl group, 3,4-di-CI,2,4-di-CI or lower C1-6 alkoxy group, the enantiomers, diastereoisomers or racemates thereof or the physiologically acceptable acid addition salts thereof which are ligands of sigma receptors for inhibiting cholesterol biosynthesis and are thus appropriate for the treatment of hypercholesterolemia and hyperlipemia in humans. The greatest lowering of cholesterol was observed by 1-(d-pyridyl)-2-(N-(2-(3,4-dicholorophenyl)ethyl-N-propylamino)ethanol in the form of dihydrobromide salt (signature BK-35. 2HBr).
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- Studies on cognitive enhancing agents. II. Antiamnestic and antihypoxic activities of 1-aryl-2-(2-aminoethoxy)ethanols
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A series of 2-(2-aminoethoxy)-1-phenylethanols having a variety of N- and phenyl-substitution patterns as well as 5- and 6-membered heteroaryl counterparts of our prototype compound 1 (2-(2-dimethylaminoethoxy)-1- phenylethanol) have been prepared and evaluated for antiamnestic and antihypoxic activities. Compound 3b, the 3-methylphenyl analogue of 1, proved to be significantly more potent than I in reversing electroconvulsive shock- induced amnesia as well as CO2-induced learning-impairment in mice. It exhibited low acute toxicity in mice and afforded a greater brain/serum concentration ratio than 1 after oral administration to rats.
- Ono,Yamafuji,Chaki,Morita,Todo,Maekawa,Kitamura,Tai,Narita
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p. 1488 - 1491
(2007/10/03)
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- A NOVEL APPROACH TO FUNCTIONALIZATION OF AZINES. OXIRANYL AND THIIRANYL DERIVATIVES OF PYRIDINE, QUINOLINE AND ISOQUINOLINE
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Convenient methods for synthesis of the oxiranyl and thiiranyl derivatives of pyridine, quinoline and isoquinoline have been elaborated.Oxiranes have been synthesized from corresponding aldehydes with dimethylsulfonium methylide in anhydrous medium.Exchange of the oxygen atom in the oxirane ring on sulfur with potassium thiocyanate gave thiiranylazines.
- Kloc, Krystian,Kubicz, Elzbieta,Mlochowski, Jacek
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p. 2517 - 2522
(2007/10/02)
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