- Highly selective hydrogenation of halogenated nitroarenes over Ru/CN nanocomposites by: In situ pyrolysis
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A highly chemoselective and recyclable ruthenium catalyst for the hydrogenation of halogenated nitroarenes has been prepared via the simple in situ calcination of a mixture of melamine, glucose and ruthenium trichloride. Superfine Ru particles (2.3 ± 0.3 nm) were obtained and highly dispersed in the nitrogen-doped carbon matrix. The Ru/CN catalyst smoothly transforms a variety of halogenated nitroarenes to the corresponding haloanilines with high intrinsic activity (e.g. TOF = 1333 h-1 for p-chloronitrobenzene) and selectivity of more than 99.6percent. Furthermore, through an analysis of the products in the reaction process, it was concluded that there are two parallel reaction pathways (a direct pathway and an indirect pathway) for the hydrogenation of aromatic nitro compounds over the Ru/CN catalyst, and the direct pathway was proved to be dominant in catalyzing the intermediates. This journal is
- Yue, Shengnan,Wang, Xueguang,Li, Shaoting,Sheng, Yao,Zou, Xiujing,Lu, Xionggang,Zhang, Chunlei
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p. 11861 - 11869
(2020/07/28)
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- COMPOUNDS AND THEIR USE AS BACE1 INHIBITORS
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The present invention relates to compounds of Formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein X, Y, Z, Q, W, m, u, ring (A), R2, R3, R4, R5 and R6, are as defined in the specification and claims. The present invention provides a pharmaceutical composition containing the compounds of Formula (I) and a therapeutic method of treating and/or preventing Downs syndrome, β-amyloid angiopathy, disorders associated with cognitive impairment, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegenerative diseases, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, Alzheimer's disease and/or Down syndrome, age-related macular degeneration (AMD), glaucoma, olfactory function impairment, traumatic brain injury, progressive muscle diseases, Type II diabetes mellitus and cardiovascular diseases (stroke).
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Page/Page column 91; 92
(2016/11/17)
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- Microwave-assisted benzyne-click chemistry: preparation of 1H-benzo[d][1,2,3]triazoles
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The benzotriazoles were prepared by three-component and two-component microwave-assisted [3+2] cycloadditions of various azides to benzyne, 3-methoxybenzyne, and 4,5-difluorobenzyne. In the three-component reaction, the aryne is generated, in the presence of an azide prepared in situ, by the reaction of an o-(trimethylsilylaryl) triflate with either CsF or KF/18-Crown-6. However, in the two-component reactions, a freshly prepared azide is added to the reaction vessel prior to aryne generation. Good to excellent yields of benzotriazoles were obtained in 15-20 min when the microwave-assisted reactions were carried out at 125 °C. These reaction times are significantly faster than similar reactions carried out using conventional heating.
- Ankati, Haribabu,Biehl, Ed
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supporting information; experimental part
p. 4677 - 4682
(2009/10/26)
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- GDC-0449-A potent inhibitor of the hedgehog pathway
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SAR for a wide variety of heterocyclic replacements for a benzimidazole led to the discovery of functionalized 2-pyridyl amides as novel inhibitors of the hedgehog pathway. The 2-pyridyl amides were optimized for potency, PK, and drug-like properties by modifications to the amide portion of the molecule resulting in 31 (GDC-0449). Amide 31 produced complete tumor regression at doses as low as 12.5 mg/kg BID in a medulloblastoma allograft mouse model that is wholly dependent on the Hh pathway for growth and is currently in human clinical trials, where it is initially being evaluated for the treatment of BCC.
- Robarge, Kirk D.,Brunton, Shirley A.,Castanedo, Georgette M.,Cui, Yong,Dina, Michael S.,Goldsmith, Richard,Gould, Stephen E.,Guichert, Oivin,Gunzner, Janet L.,Halladay, Jason,Jia, Wei,Khojasteh, Cyrus,Koehler, Michael F.T.,Kotkow, Karen,La, Hank,LaLonde, Rebecca L.,Lau, Kevin,Lee, Leslie,Marshall, Derek,Marsters Jr., James C.,Murray, Lesley J.,Qian, Changgeng,Rubin, Lee L.,Salphati, Laurent,Stanley, Mark S.,Stibbard, John H.A.,Sutherlin, Daniel P.,Ubhayaker, Savita,Wang, Shumei,Wong, Susan,Xie, Minli
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scheme or table
p. 5576 - 5581
(2010/04/05)
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- QUINOXALINE INHIBITORS OF THE HEDGEHOG SIGNALLING PATHWAY
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The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I wherein A is a carbocycle or heterocycle; X is alkylene, NR4C(O), NR
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Page/Page column 43; 44
(2008/06/13)
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- 3-aryluracil derivatives and their use for weed control
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3-Aryluracil derivatives of the formula I STR1 in which --W-- is the group STR2 where the ring nitrogen atom is bonded via the C atom; R1 is hydrogen, C1 -C4 alkyl, C1 -C4 haloalkyl, C3 alkenyl or C4 alkenyl or C3 alkynyl or C4 alkynyl; R2 is halogen or cyano; R3 is hydrogen or halogen; R4 is hydrogen, halogen or C1 -C4 alkyl; R5 is C1 -C4 alkyl or C1 -C4 haloalkyl; or R4 and R5 together are --(CH2)n --; n is the number 3 or 4; R13 is C1 -C4 alkyl, C3 alkenyl or C4 alkynyl or C3 alkynyl or C4 alkynyl; and Q is one of the groups a) to e): STR3 where R6 to R12 are substituents, m is 3, 4 or 5, X is oxygen or sulfur and t is 2, 3 or 4, and if R1 is hydrogen, the agrochemically acceptable salts of compounds of the formula I. the compounds of formula I have herbicidal properties and are suitable as the active ingredient in a herbicide.
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- THE SYNTHESIS OF TWO STRONGLY ELECTRON DEFICIENT FLAVIN ANALOGS
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The synthesis of 7-chloro-8-acetyl-10-methylisoalloxazine (2a) and 7-cyano-8-acetyl-10-methylisoalloxazine (2b) was accomplished by the condensation of appropriately substituted o-diamines with alloxan under acidic conditions.The presence of the strongly
- Radziejewski, Czeslaw,Ghosh, Soumitra,Kaiser, Emil Thomas
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p. 1227 - 1238
(2007/10/02)
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