- Using DMF as Both a Catalyst and Cosolvent for the Regioselective Silylation of Polyols and Diols
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Highly regioselective silylation of primary hydroxyl groups of unprotected polyols and diols was obtained by the use of a mixed solvent of MeCN/DMF (10:1) in this study. DMF was discovered to be a good catalyst in this reaction, although the silylation us
- Lv, Jian,Luo, Tao,Zou, Dapeng,Dong, Hai
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p. 6383 - 6395
(2019/11/05)
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- TRIAZOLOPYRIDINE INHIBITORS OF MYELOPEROXIDASE
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The present invention provides compounds of Formula (I): wherein A is as defined in the specification, and compositions comprising any of such novel compounds. These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments.
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Paragraph 00387
(2017/03/28)
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- Synthesis and Applications of Silyl 2-Methylprop-2-ene-1-sulfinates in Preparative Silylation and GC-Derivatization Reactions of Polyols and Carbohydrates
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Trimethylsilyl, triethylsilyl, tert-butyldimethylsilyl, and triisopropylsilyl 2-methylprop-2-ene-1-sulfinates were prepared through (CuOTf)2C6H6-catalyzed sila-ene reactions of the corresponding methallylsilanes with SO2 at 50 °C. Sterically hindered, epimerizable, and base-sensitive alcohols gave the corresponding silyl ethers in high yields and purities at room temperature and under neutral conditions. As the byproducts of the silylation reaction (SO2+isobutylene) are volatile, the workup was simplified to solvent evaporation. The developed method can be employed for the chemo- and regioselective semiprotection of polyols and glycosides and for the silylation of unstable aldols. The high reactivity of the developed reagents is shown by the synthesis of sterically hindered per-O-tert-butyldimethylsilyl-α-d-glucopyranose, the X-ray crystallographic analysis of which is the first for a per-O-silylated hexopyranose. The per-O-silylation of polyols, hydroxy carboxylic acids, and carbohydrates with trimethylsilyl 2-methylprop-2-ene-1-sulfinate was coupled with the GC analysis of nonvolatile polyhydroxy compounds both qualitatively and quantitatively. Regio- and chemoselective silylation of polyols and carbohydrates has been achieved by employing silyl sulfinates (see the picture; TBS=tert-butyldimethylsilyl, TES=triethylsilyl, TIPS=triisopropylsilyl, TMS=trimethylsilyl). The silylation reactions proceed in high yield because the reactions are mild and fast and produce only volatile byproducts. Furthermore, the silyl sulfinates are used as new derivatization reagents for the GC analysis of nonvolatile polyhydroxy compounds.
- Markovic, Dean,Tchawou, Wandji Augustin,Novosjolova, Irina,Laclef, Sylvain,Stepanovs, Dmitrijs,Turks, Maris,Vogel, Pierre
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p. 4196 - 4205
(2016/03/16)
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- Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2
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Using structure-based design, a novel series of pyridone ERK1/2 inhibitors was developed. Optimization led to the identification of (S)-14k, a potent, selective, and orally bioavailable agent that inhibited tumor growth in mouse xenograft models. On the basis of its in vivo efficacy and preliminary safety profiles, (S)-14k was selected for further preclinical evaluation.
- Ren, Li,Grina, Jonas,Moreno, David,Blake, James F.,Gaudino, John J.,Garrey, Rustam,Metcalf, Andrew T.,Burkard, Michael,Martinson, Matthew,Rasor, Kevin,Chen, Huifen,Dean, Brian,Gould, Stephen E.,Pacheco, Patricia,Shahidi-Latham, Sheerin,Yin, Jianping,West, Kristina,Wang, Weiru,Moffat, John G.,Schwarz, Jacob B.
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p. 1976 - 1991
(2015/04/27)
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- PYRIMIDONE DERIVATIVES USED AS TAU PROTEIN KINASE 1 INHIBITORS
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A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C-X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1 -C3 alkyl group; L represents single bond or a C1 -C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
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Page/Page column 43
(2011/02/24)
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- Silyl methallylsulfinates: Efficient and powerful agents for the chemoselective silylation of alcohols, polyols, phenols and carboxylic acids
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Alcohols, phenols and carboxylic acids are silylated with very good yields in the presence of silyl methallylsulfinates under non-basic conditions and with the formation of volatile co-products. The Royal Society of Chemistry 2005.
- Huang, Xiaogen,Craita, Cotinica,Awad, Loay,Vogel, Pierre
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p. 1297 - 1299
(2008/03/28)
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- 6-substituted amino-4-oxa-1-azabicyclo[3.2.0]heptan-7-one derivatives as cysteine protease inhibitors
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Novel 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one compounds, as well as the pharmaceutically acceptable salts thereof and diastereoisomers thereof, of formula I, are disclosed, which exhibit excellent cysteine protease inhibitory activity and may be used for treatment of different diseases such as muscular dystrophy, arthritis, myocardial infarction, Alzheimer's disease, bacterial infection, common cold, osteroporosis and cancer metastasis.
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- Enantioselective synthesis of α-hydroxyacids through oxidation of terminal alkenes with AD-mix/TEMPO
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α-Hydroxyacids can be enantioselectively prepared by means of a two- step oxidation process, involving first the asymmetric dihydroxylation of a terminal alkene and subsequent oxidation with TEMPO/NaOCl/NaClO2 in good to excellent yields. No fragmentation of the glycol intermediate was detected. (C) 2000 Elsevier Science Ltd.
- Javier Aladro,Guerra, Francisco M.,Javier Moreno-Dorado,Bustamante, Jesús M.,Jorge, Zacarías D.,Massanet, Guillermo M.
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p. 3209 - 3213
(2007/10/03)
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- Acid-catalyzed solvolysis of polyenol ethers. III. Effect of the alkoxy moiety
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The dependence of the solvolysis of polyenol ethers on the nature of the alkoxy moiety has been studied. A new reaction path, leading to the formation of ω-hydroxy (methoxy) substituted aldehydes and -esters, was established. The proposed reaction pathway (scheme 6) is initiated by an electron transfer from the polyenol ether to molecular oxygen, followed by combination of the two radicals to a peroxide zwitterion. Upon protonation, solvent adds to the ω-carbon atom of the polyene to give an intermediate that can either loose water to form an ester, or loose the alkoxy moiety to give an aldehyde. This mechanism is believed to be involved in the strong mutagenic activity displayed by many polyenol ethers, including the natural mutagen fecapentaene-12.
- Nieuwenhuis, Saskia A. M.,Vertegaal, Louis B. J.,De Zoete, Marian C.,Van Der Gen, Arne
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p. 13207 - 13230
(2007/10/02)
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- Kinetically Controlled Regiospecific Silylation of Polyols via Dibutylstannanediyl Acetals
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A general procedure is described whereby the tert-butyldimethylsilylation of unsymmetrical 1,2- and 1,3-diols via their dibutylstannanediyl derivatives occurs regiospecifically at the primary hydroxy group under neutral conditions; six-membered ring aceta
- Leigh, David A.,Martin, Richard P.,Smart, John P.,Truscello, Ada M.
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p. 1373 - 1374
(2007/10/02)
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- The Utility of t-Butyldimethylsilane as an Effective Silylation Reagent for the Protection of Functional Groups
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Treatment of compounds containing functional groups, such as alcohols, amines, and carboxylic acids, with t-butyldimethylsilane in the presence of a catalytic amount of palladium on carbon is described to provide a new, convenient method for the introduction of a t-butyldimethylsilyl (TBDMS) group.
- Yamamoto, Keiji,Takemae, Makoto
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p. 2111 - 2113
(2007/10/02)
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