- Nickel-Catalyzed Cross-Coupling of Functionalized Organo manganese Reagents with Aryl and Heteroaryl Halides Promoted by 4-Fluorostyrene
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A catalytic system consisting of Ni(acac) 2 (5 mol%) and 4-fluorostyrene (20 mol%) allows a convenient cross-coupling of functionalized organomanganese reagents with a variety of aryl and heteroaryl halides leading to polyfunctionalized diaryl- and arylheteroarylmethane derivatives.
- Benischke, Andreas D.,Desaintjean, Alexandre,Juli, Thomas,Cahiez, Gérard,Knochel, Paul
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supporting information
p. 5396 - 5412
(2017/12/14)
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- IMPROVEMENTS IN OR RELATING TO ORGANIC COMPOUNDS
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An aryl-substituted alkanal compound having a molecular weight of less than 300 g/mol and which bears a substituent on the aryl ring ortho to a substituent bearing the aldehyde functionality. Said compounds are useful as perfume ingredients in personal ca
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Page/Page column 44-45
(2014/12/09)
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- AMINE LINKED MODULATORS OF y-SECRETASE
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The present invention relates to compounds of Formula I as shown below, wherein the definitions of A, X, Y, R1 R2, R3, R4, R5, R6, R7, R8, and R9 are provided in the specification. Compounds of Formula I are useful for the treatment of diseases associated with γ-secretase activity, including Alzheimer's disease.
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Page/Page column 37
(2009/05/29)
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- GSM INTERMEDIATES
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The present invention relates the use of compounds having the general Formula I, wherein the definitions or R1 and R2 are provided in the specification. Said compounds of Formula I are useful for the synthesis of a variety of g-secretase modulators, which are in turn useful for the treatment of diseases associated with y-secretase activity, including Alzheimer′s disease.
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Page/Page column 123-124; 149-150
(2009/05/28)
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- METABOLICALLY STABLE ALKOXYALKYL ESTERS OF ANTIVIRAL OR ANTIPROLIFERATIVE PHOSPHONATES, NUCLEOSIDE PHOSPHONATES AND NUCLEOSIDE PHOSPHATES
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The present invention relates to phosphonate, nucleoside phosphonate or nucleoside phosphate compounds, compositions containing them, processes for obtaining them, and their use in treating a variety of medical disorders, in particular viral infections, cancers and the like.
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Page/Page column 25
(2008/06/13)
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- Compositions useful as inhibitors of protein kinases
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The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides processes for preparing the compounds, pharmaceutically acceptable compositions comprising the compounds, and methods of using the compounds and compositions in the treatment of various disease, conditions, or disorders.
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Page/Page column 109
(2008/06/13)
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- An ESR and HPLC-EC assay for the detection of alkyl radicals
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The correlation of lipid peroxidation with release of alkanes (RH) is considered a noninvasive method for the in vivo evaluation of oxidative stress. The formation of RH is believed to reflect a lipid hydroperoxide (LOOH)-dependent generation of alkoxyl radicals (LO·) that undergo β-scission with release of alkyl radicals (R·). Alternatively, R· could be spin-trapped with a nitrone before the formation of RH and analyzed by ESR. Extracts from the liver and lung of CCl4- and asbestos-treated rats that were previously loaded with nitrones exhibited ESR spectra suggesting the formation of iso-propyl, n-butyl, ethyl, and pentyl radical-derived nitroxides. In biological systems, various nitroxides with indistinguishable ESR spectra could be formed. Hence, experiments with N-tert-butyl-α-phenylnitrone (PBN) for spin trapping of R· were carried out in which the nitroxides formed were separated and analyzed by HPLC with electrochemical detection (EC). The C1-5 homologous series of PBN nitroxides and hydroxylamines were synthesized, characterized by ESR, GC-MS, and HPLC-EC, and used as HPLC standards. For in vivo generation and spin trapping of R·, rats were loaded with CCl4 and PBN. The HPLC-EC chromatograms of liver extracts from CCl4-treated rats demonstrated the formation of both the nitroxide and hydroxylamine forms of PBN/·CCl3, as well as the formation of a series of unidentified PBN nitroxides and hydroxylamines. However, formation of PBN adducts with retention times similar to these of the PBN/C2-5 derivatives was not observed. In conclusion, we could not correlate the production of PBN-detectable alkyl radicals with the reported CCl4-dependent production of C1-5 alkanes. We speculate that the major reason for this is the low steady-state concentrations of R· produced because only a small fraction of LO· undergo β-scission to release R·.
- Novakov,Feierman,Cederbaum,Stoyanovsky
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p. 1239 - 1246
(2007/10/03)
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- Prostaglandin endoperoxide H synthase biosynthesis inhibitors
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The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).
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- New syntheses of the rice moth and stink bug pheromones by employing (2R, 6S)-7-acetoxy-2,6-dimethyl-1-heptanol as a building block
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(2R, 6R, 10R)-6,10,14-Trimethyl-2-pentadecanol, the female pheromone of the rice moth (Corcyra cephalonica), and methyl (2R, 6R, 10R)-2,6,10-trimethyltridecanoate, the male pheromone of the stink bug (Euschistus heros) were synthesized by employing (2R, 6S)-7-acetoxy-2,6-dimethyl-1-heptanol as the common chiral building block.
- Nakamura, Yoshihide,Mori, Kenji
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p. 1713 - 1721
(2007/10/03)
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- 1,2-Induction in intramolecular diene cyclozirconation: Control of relative configuration
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We have observed that cyclozirconation of a diene having a substituent on the bridge connecting the two alkene leads to a single predominant zirconacycle with control of three new stereogenic centers.
- Taber, Douglass F.,Louey, James P.
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p. 4495 - 4506
(2007/10/02)
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- Process for the preparation of terpenes
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A terpene compound having the formula (III) is produced by reacting an allylic halide having the formula (I) with a Grignard reagent having the formula (II) in the presence of anhydrous zinc chloride and a copper compound or an organic zinc halide compound having the formula (IV) in the presence of a copper compound, provided that when A-A is C-C, R' is hydrogen and when A-A is C=C, X is chlorine. STR1
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- New Histidyl amino acid derivatives, and pharmaceutical composition comprising the same
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A compound of the formula: STR1 wherein R1 is lower alkyl optionally substituted with a substituent selected from the group consisting of acyl, hydroxy, lower alkoxy, aryl, lower alkylthio and a group of the formula: STR2 in which R5 is hydrogen or acyl and R6 is hydrogen or lower alkyl; aryl; or amino optionally substituted with substituent(s) selected from the group consisting of lower alkyl and acyl; and R2 is hydrogen or lower alkyl; or R1 and R2 are taken together with the attached nitrogen atom to form a heterocyclic group optionally substituted with substituent(s) selected from the group consisting of lower alkyl, hydroxy(lower )alkyl, lower alkoxy(lower)alkyl, acyl(lower)alkyl, oxo and acyl; R3 is hydrogen or lower alkyl; and R4 is lower alkyl; and its pharmaceutically acceptable salt, processes for the preparation thereof and pharmaceutical composition comprising the same.
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- RENIN INHIBITOR PEPTIDE COMPOUNDS, A PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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A compound of the formula: STR1 wherein R 1 is aryl optionally substituted with a substituent selected from the group consisting of halogen and halo(lower)alkyl; lower alkyl or cyclo(lower) alkyl; andR 2 is hydrogen or lower alkyl, or R. sup.1 and R 2 are taken together with the attached nitrogen atom to form a heterocyclic group optionally substituted with a substituent selected from the group consisting of lower alkyl and esterified carboxy, R 3 is hydrogen or lower alkyl, andR 4 is lower alkyl,and its pharmaceutically acceptable salt, a process for the preparation thereof and pharmaceutical composition comprising the same.
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- 2,6,10-TRIMETHYL-7-(3-METHYLBUTYL)-DODECANE, A NOVEL SEDIMENTARY BIOLOGICAL MARKER COMPOUND.
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A C20 isoprenoid alkane (1) reported to occur in several recent sediments, has been isolated from Rozel Point crude oil and its structure confirmed by synthesis.
- Yon, D.A.,Maxwell, J.R.,Ryback, G.
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p. 2143 - 2146
(2007/10/02)
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- Benzaldehydes, alkanophenones, and benzophenones and derivatives thereof containing a 4-monoalkylamino group
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Novel 4-monoalkylamino-benzaldehydes, 4-mono-alkylamino-alkanophenones, and 4-monoalkylamino-benzophenones, and derivatives and salts thereof, are disclosed which are useful as anti-atherosclerotic agents.
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- 4-(Monoalkylamino) benzene polycarboxylic acids
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This disclosure describes the monoalkylaminobenzene multi-carboxylic acids, derivatives and salts thereof useful as hypolipidemic and anti-atherosclerotic agents.
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