- Microwave-assisted reduction of aromatic nitro compounds with novel oxo-rhenium complexes
-
The reduction of several aromatic nitro compounds to amines by means of the two novel catalytic systems ([IMes]2ReOBr3)/PhSiH3 and ([Py]3ReNOBr2)/PhSiH3 under microwave irradiation is here reported. These two systems were able to perform the reduction of nitro groups with higher TON and TOF when compared with previously reported systems based on oxo-rhenium core under standard heating, although they showed a lesser broad reaction scope compared with the known systems.
- Grieco, Gabriele,Blacque, Olivier
-
-
- Cobalt nanoclusters coated with N-doped carbon for chemoselective nitroarene hydrogenation and tandem reactions in water
-
The development of active and selective non-noble metal-based catalysts for the chemoselective reduction of nitro compounds in aquo media under mild conditions is an attractive research area. Herein, the synthesis of subnanometric and stable cobalt nanoclusters, covered by N-doped carbon layers as core-shell (Co@NC-800), for the chemoselective reduction of nitroarenes is reported. TheCo@NC-800catalyst was prepared by the pyrolysis of the Co(tpy)2complex impregnated on Vulcan carbon. In fact, the use of a molecular complex based on six N-Co bonds drives the formation of a well-defined and distributed cobalt core-shell nanocluster covered by N-doped carbon layers. In order to elucidate its nature, it has been fully characterized by using several advanced techniques. In addition, this as-prepared catalyst showed high activity, chemoselectivity and stability toward the reduction of nitro compounds with H2and under mild reaction conditions; water was used as a green solvent, improving the previous results based on cobalt catalysts. Moreover, theCo@NC-800catalyst is also active and selective for the one-pot synthesis of secondary aryl amines and isoindolinones through the reductive amination of nitroarenes. Finally, based on diffraction and spectroscopic studies, metallic cobalt nanoclusters with surface CoNxpatches have been proposed as the active phase in theCo@NC-800material.
- Agostini, Giovanni,Calvino, Jose. J.,Corma, Avelino,Gutiérrez-Tarri?o, Silvia,Lopes, Christian W.,O?a-Burgos, Pascual,Rojas-Buzo, Sergio
-
supporting information
p. 4490 - 4501
(2021/06/28)
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- Commercially Available CuO Catalyzed Hydrogenation of Nitroarenes Using Ammonia Borane as a Hydrogen Source
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Tandem ammonia borane dehydrogenation and nitroarenes hydrogenation has been reported as a novel strategy for the preparation of aromatic amines. However, the practical application of this strategy is subjected to the high-cost and tedious preparation of supported noble metal nanocatalysts. The commercially available CuO powder is herein demonstrated to be a robust catalyst for hydrogenation of nitroarenes using ammonia borane as a hydrogen source under mild conditions. Numerous amines (even sterically hindered, halogenated, and diamines) could be obtained through this method. This monometallic catalyst is characteristic of support-free, excellent chemoselectivity, low-cost, and high recyclability, which will favor its future utilization in preparative reduction chemistry. Mechanistic studies are also carried out to clarify that diazene and azoxybenzene are key intermediates of this heterogeneous reduction.
- Du, Jialei,Chen, Jie,Xia, Hehuan,Zhao, Yiwei,Wang, Fang,Liu, Hong,Zhou, Weijia,Wang, Bin
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p. 2426 - 2430
(2020/03/30)
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- Synthesis of water soluble Pd-Piperidoimidazolin-2-ylidene complexes and their catalytic activities in neat water
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Through the strategy of water soluble N-heterocyclic carbene (NHC) ligand, Pd-catalyzed reactions were developed in aqueous media. Therefore, four new piperidoimidazolinium salts (1a-d) consisting of sulfonate (a), esther (b, c) and carboxylic acid (d) functionalities and their water-soluble Pd-NHC complexes (2a-d) were synthesized. The new compounds were characterized by elemental analysis, FTIR, TGA, UV–vis and NMR spectroscopy. The catalytic activities of water soluble Pd-NHC complexes (2a-d) were investigated using the Suzuki-Miyaura (S-M) reaction and the reduction of nitroarenes. We found that the water-soluble polar or ionic groups on piperidoimidazolin-2-ylidine had an effect on the catalytic activity. The water-soluble catalyst can be recycled efficiently and reused six times with only a very slight loss of catalytic activity.
- ?ak?r, Sinem,Türkmen, Hayati
-
-
- Defect-mediated selective hydrogenation of nitroarenes on nanostructured WS2
-
Transition metal dichalcogenides (TMDs) are well known catalysts as both bulk and nanoscale materials. Two-dimensional (2-D) TMDs, which contain single- and few-layer nanosheets, are increasingly studied as catalytic materials because of their unique thickness-dependent properties and high surface areas. Here, colloidal 2H-WS2 nanostructures are used as a model 2-D TMD system to understand how high catalytic activity and selectivity can be achieved for useful organic transformations. Free-standing, colloidal 2H-WS2 nanostructures containing few-layer nanosheets are shown to catalyze the selective hydrogenation of a broad scope of substituted nitroarenes to their corresponding aniline derivatives in the presence of other reducible functional groups. Microscopic and computational studies reveal the important roles of sulfur vacancy-rich basal planes and tungsten-terminated edges, which are more abundant in nanostructured 2-D materials than in their bulk counterparts, in enabling the functional group selectivity. At tungsten-terminated edges and on regions of the basal planes having high concentrations of sulfur vacancies, vertical adsorption of the nitroarene is favored, thus facilitating hydrogen transfer exclusively to the nitro group due to geometric effects. At lower sulfur vacancy concentrations on the basal planes, parallel adsorption of the nitroarene is favored, and the nitro group is selectively hydrogenated due to a lower kinetic barrier. These mechanistic insights reveal how the various defect structures and configurations on 2-D TMD nanostructures facilitate functional group selectivity through distinct mechanisms that depend upon the adsorption geometry, which may have important implications for the design of new and enhanced 2-D catalytic materials across a potentially broad scope of reactions.
- Sun, Yifan,Darling, Albert J.,Li, Yawei,Fujisawa, Kazunori,Holder, Cameron F.,Liu, He,Janik, Michael J.,Terrones, Mauricio,Schaak, Raymond E.
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p. 10310 - 10317
(2019/11/20)
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- One-pot formic acid dehydrogenation and synthesis of benzene-fused heterocycles over reusable AgPd/WO2.72 nanocatalyst
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Using nanoparticles (NPs) to catalyze multiple chemical reactions in one-pot and to achieve high-yield syntheses of functional molecules/materials is an important direction in NP chemistry, catalysis and applications. In this article, we report a nanocomposite of AgPd NPs anchored on WO2.72 nanorods (NRs) (denoted as AgPd/WO2.72) as a general catalyst for formic acid dehydrogenation and transfer hydrogenation from Ar-NO2 to Ar-NH2 that further reacts with aldehydes to form benzene-fused heterocyclic compounds. The AgPd/WO2.72 catalysis is Ag/Pd dependent and Ag48Pd52 is the most active composition for the multiple chemical reactions. The high activity of AgPd/WO2.72 arises from strong interfacial interaction between AgPd and WO2.72, resulting in AgPd lattice expansion and electron polarization from AgPd to WO2.72. The syntheses proceed in one-pot reactions among formic acid, 2-nitrophenol (or 2-nitroaniline, or 2-nitrothiophenol) and aldehydes in dioxane/water (2/1 v/v) at 80-90 °C, leading to one-pot syntheses of benzoxazoles, benzimidazoles and benzothiazoles that are key ring structures present in functional compounds for pharmaceutical, optical and polymer applications.
- Yu, Chao,Guo, Xuefeng,Shen, Bo,Xi, Zheng,Li, Qing,Yin, Zhouyang,Liu, Hu,Muzzio, Michelle,Shen, Mengqi,Li, Junrui,Seto, Christopher T.,Sun, Shouheng
-
supporting information
p. 23766 - 23772
(2018/12/10)
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- A capping agent dissolution method for the synthesis of metal nanosponges and their catalytic activity towards nitroarene reduction under mild conditions
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We report a general strategy for the synthesis of metal nanosponges (M = Ag, Au, Pt, Pd, and Cu) using a capping agent dissolution method where addition of water to the M@BNHx nanocomposite affords the metal nanosponges. The B-H bond of the BNHx polymer gets hydrolysed upon addition of water and produces hydrogen gas bubbles which act as dynamic templates leading to the formation of nanosponges. The rate of B-H bond hydrolysis has a direct impact on the final nanostructure of the materials. The metal nanosponges were characterized using powder XRD, electron microscopy, XPS, and BET surface area analyzer techniques. The porous structure of these nanosponges offers a large number of accessible surface sites for catalytic reactions. The catalytic activity of these metal nanosponges has been demonstrated for the reduction of 4-nitrophenol where palladium exhibits the highest catalytic activity (k = 0.314 min?1). The catalytic activity of palladium nanosponge was verified for the tandem dehydrogenation of ammonia borane and the hydrogenation of nitroarenes to arylamines in methanol at room temperature. The reduction of various substituted nitroarenes was proven to be functional group tolerant except for a few halogenated nitroarenes (X = Br and I) and >99% conversion was noted within 30-60 min with high turnover frequencies (TOF) at low catalyst loading (0.1 mol%). The catalyst could be easily separated out from the reaction mixture via centrifugation and was recyclable over several cycles, retaining its porous structure.
- Ghosh, Sourav,Jagirdar, Balaji R.
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p. 17401 - 17411
(2019/01/03)
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- Base metal-catalyzed benzylic oxidation of (aryl)(heteroaryl)methanes with molecular oxygen
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The methylene group of various substituted 2- and 4-benzylpyridines, benzyldiazines and benzyl(iso)quinolines was successfully oxidized to the corresponding benzylic ketones using a copper or iron catalyst and molecular oxygen as the stoichiometric oxidant. Application of the protocol in API synthesis is exemplified by the alternative synthesis of a precursor to the antimalarial drug Mefloquine. The oxidation method can also be used to prepare metabolites of APIs which is illustrated for the natural product papaverine. ICP-MS analysis of the purified reaction products revealed that the base metal impurity was well below the regulatory limit.
- Sterckx, Hans,De Houwer, Johan,Mensch, Carl,Herrebout, Wouter,Tehrani, Kourosch Abbaspour,Maes, Bert U.W.
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supporting information
p. 144 - 153
(2016/04/05)
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- A metal-organic framework-templated synthesis of γ-Fe2O3 nanoparticles encapsulated in porous carbon for efficient and chemoselective hydrogenation of nitro compounds
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The γ-Fe2O3 nanoparticles well dispersed in porous carbon were fabricated via a Fe-based metal-organic framework-templated pyrolysis. The resultant product exhibits excellent catalytic activity, chemoselectivity and magnetic recyclability for the hydrogenation of diverse nitro compounds under mild conditions.
- Li, Yang,Zhou, Yu-Xiao,Ma, Xiao,Jiang, Hai-Long
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supporting information
p. 4199 - 4202
(2016/03/19)
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- Immobilized iron oxide nanoparticles as stable and reusable catalysts for hydrazine-mediated nitro reductions in continuous flow
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An experimentally easy to perform method for the generation of alumina-supported Fe3O4 nanoparticles [(6±1)nm size, 0.67 wt%]and the use of this material in hydrazine-mediated heterogeneously catalyzed reductions of nitroarenes to anilines under batch and continuous-flow conditions is presented. The bench-stable, reusable nano-Fe3O4@Al2O3 catalyst can selectively reduce functionalized nitroarenes at 1 mol% catalyst loading by using a 20 mol% excess of hydrazine hydrate in an elevated temperature regime (150°C, reaction time 2-6 min in batch). For continuous-flow processing, the catalyst material is packed into dedicated cartridges and used in a commercially available high-temperature/-pressure flow device. In continuous mode, reaction times can be reduced to less than 1 min at 150°C (30 bar back pressure) in a highly intensified process. The nano-Fe3O4@Al2O3 catalyst demonstrated stable reduction of nitrobenzene (0.5 m in MeOH) for more than 10 h on stream at a productivity of 30mmolh-1 (0.72 mol per day). Importantly, virtually no leaching of the catalytically active material could be observed by inductively coupled plasma MS monitoring.
- Moghaddam, Mojtaba Mirhosseini,Pieber, Bartholom?us,Glasnov, Toma,Kappe, C. Oliver
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p. 3122 - 3131
(2015/09/28)
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- NAMPT INHIBITORS
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Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.
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Page/Page column 167; 225
(2013/12/03)
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- Hydrazine-mediated reduction of nitro and azide functionalities catalyzed by highly active and reusable magnetic iron oxide nanocrystals
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Iron oxide (Fe3O4) nanocrystals generated in situ from an inexpensive and readily available iron source catalyze the reduction of nitroarenes to anilines with unparalleled efficiency. The procedure is chemoselective, avoids the use of precious metals, and can be applied under mild reflux conditions (65 or 80 C) or using sealed vessel microwave heating in an elevated temperature regime (150 C). Utilizing microwave conditions, a variety of functionalized anilines have been prepared in nearly quantitative yields within 2-8 min at 150 C, in a procedure also successfully applied to the reduction of aliphatic nitro compounds and azides. The iron oxide nanoparticles are generated in a colloidal form, resulting in homogeneous solutions suitable for continuous flow processing. Selected examples of anilines of industrial importance have been prepared in a continuous regime using this protocol.
- Cantillo, David,Moghaddam, Mojtaba Mirhosseini,Kappe, C. Oliver
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p. 4530 - 4542
(2013/06/05)
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- Design, synthesis and characterization of N', N''- Diaryl ureas as p38 kinase inhibitors
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Kinases have been known as important molecular targets for various diseases and p38 kinase is found to be vital target among all mitogen activated protein kinases for inflammatory diseases. P38 kinase inhibitors bearing urea scaffold have shown potent kinase inhibitory activity and also selectivity over other kinases. We present here the synthesis, p38 kinase inhibitory and anti-inflammatory activities of compounds containing N', N''-diarylurea scaffold. Compound 7f demonstrated IC50 value of 1.09 μM in p38 kinase assay and 79.41% inhibition of rat paw edema at the 2nd hour of carrageenan challenge. The molecular docking studies of synthesized compounds indicated some of the important hydrogen bonding interactions and also revealed the minor change in the binding pose when compared to BIRB796.
- Kulkarni, Ravindra G.,Laufer, Stefan,Mangannavar, Chandrashekhar,Garlapati, Achaiah
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p. 213 - 221
(2013/07/28)
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- In situ generated iron oxide nanocrystals as efficient and selective catalysts for the reduction of nitroarenes using a continuous flow method
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The best of both worlds: The benefits of homogeneous and heterogeneous nanocatalysis are combined, whereby highly reactive colloidal Fe 3O4 nanocrystals are generated in situ that remain in solution long enough to allow the efficient and selective reduction of nitroarenes to anilines in continuous-flow mode (see scheme). After completion of the reaction, the nanoparticles aggregate and can be recovered by a magnet. Copyright
- Cantillo, David,Baghbanzadeh, Mostafa,Kappe, C. Oliver
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p. 10190 - 10193
(2012/11/07)
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- INHIBITION OF P38 KINASE ACTIVITY USING SUBSTITUTED HETEROCYCLIC UREAS
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This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.
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Page/Page column 16-17
(2012/03/10)
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- Inhibition Of Raf Kinase Using Symmetrical And Unsymmetrical Substituted Diphenyl Ureas
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This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
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Page/Page column 13
(2008/12/04)
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- Affinity of 3-acyl substituted 4-quinolones at the benzodiazepine site of GABAA receptors
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The finding that alkyl 1,4-dihydro-4-oxoquinoline-3-carboxylate and N-alkyl-1,4-dihydro-4-oxoquinoline-3-carboxamide derivatives may be high-affinity ligands at the benzodiazepine binding site of the GABAA receptor, prompted a study of 3-acyl-1,4-dihydro-4-oxoquinoline (3-acyl-4-quinolones). In general, the affinity of the 3-acyl derivatives was found to be comparable with the 3-carboxylate and the 3-carboxamide derivatives, and certain substituents (e.g., benzyl) in position 6 were again shown to be important. As it is believed that the benzodiazepine binding site is situated between an α- and a γ-subunit in the GABAA receptor, selected compounds were tested on the α1β2γ2s, α2β2γ2s and α3β2γ2s GABAA receptor subtypes. The 3-acyl-4-quinolones display various degrees of selectivity for α1- versus α2- and α3-containing receptors, and high-affinity ligands essentially selective for α1 over α3 were developed.
- Lager, Erik,Nilsson, Jakob,stergaard Nielsen, Elsebet,Nielsen, Mogens,Liljefors, Tommy,Sterner, Olov
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p. 6936 - 6948
(2008/12/21)
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- INHIBITION OF RAF KINASE USING SUBSTITUTED HETEROCYCLIC UREAS
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Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.
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Page/Page column 16-17
(2010/11/28)
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- Phenoxypiperidines and analogs thereof useful as histamine H3 antagonists
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Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(═O)—, —C(═NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combination with other agents.
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Page/Page column 50-51
(2010/11/27)
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- Cinnamide and hydrocinnamide derivatives with kinase inhibitory activity
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The present invention provides novel cinnamide compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
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Page/Page column 176
(2008/06/13)
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- Palladium-catalyzed silane/siloxane reductions in the one-pot conversion of nitro compounds into their amines, hydroxylamines, amides, sulfonamides, and carbamates
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A combination of palladium(II) acetate, aqueous potassium fluoride, and polymethylhydrosiloxane (PMHS) facilitates the room-temperature reduction of aromatic nitro compounds to anilines. These reactions tend to be quick (30 min), high-yielding, and tolerate a range of other functional groups. Replacement of PMHS/KF with triethylsilane allows for the reduction of aliphatic nitro compounds to their corresponding hydroxylamines. Depending on the substrate, both conditions can allow for the in situ conversion of the product amines into amides, sulfonamides, and carbamates. Georg Thieme Verlag Stuttgart.
- Rahaim Jr., Ronald J.,Maleczka Jr., Robert E.
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p. 3316 - 3340
(2008/09/17)
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- BENZIMIDAZOLE CARBOXAMIDES AS RAF KINASE INHIBITORS
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The present invention relates to benzimidazole carboxamides of formula (I), the use of the compounds of formula (I) as inhibitors of as inhibitors of one or more kinases, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient. Accordingly, the compound of Formula (I) or a pharmaceutically acceptable salt thereof is administered for the treatment of diseases mediated by one or more kinase phathways, preferably by the raf kinase pathway, especially cancers.
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Page/Page column 131
(2008/06/13)
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- MALONAMIDE DERIVATIVES
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The present invention relates to malonamide derivatives of formula (I): A-D-B, the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.
- -
-
-
- INHIBITION OF p38 KINASE USING SYMMETRICAL AND UNSYMMETRICAL DIPHENYL UREAS
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This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.
- -
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Page/Page column 26
(2010/02/11)
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- Substituted indolines which inhibit receptor tyrosine kinases
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Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone, (b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and (c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
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Page column 50
(2008/06/13)
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- Development of a continuous-flow system for catalysis with palladium(0) particles
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Heterogeneous catalysis for organic synthesis under continuous-flow conditions becomes possible by a new reactor-based approach. Continuous-flow reactors with a monolithic glass/polymer composite interior are loaded with palladium particles by ion exchange followed by reduction. When incorporated into a continuous-flow setup (PASSflow) this reactor allows the transfer-hydrogenation of alkenes, alkynes, nitro-substituted aromatic compounds and benzyl ethers in the flow-through mode. In addition, the activity of the catalysts is well suited to achieve Suzuki, Sonogashira and Heck cross-coupling reactions in the absence of phosphanes or any other ligands, resulting in a greatly simplified purification. As an extension to this concept a bifunctional support was prepared inside the reactor consisting of Pd particles and an ion-exchange group (hydroxide form). In the Suzuki-Miyaura reaction the reactor serves as a base for immobilisation and activation of the boronic acid as boronate and as a catalyst for promoting the C-C coupling reaction under continuous-flow conditions. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
- Solodenko, Wladimir,Wen, Hongliang,Leue, Stefanie,Stuhlmann, Friedrich,Sourkouni-Argirusi, Georgia,Jas, Gerhard,Schoenfeld, Hagen,Kunz, Ulrich,Kirschning, Andreas
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p. 3601 - 3610
(2007/10/03)
-
- Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
-
This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.
- -
-
-
- Inhibition of raf kinase using symmetrical and unsymmetrical substituted diphenyl ureas
-
This invention relates to the use of a group of aryl ureas in treating raf mediated diseases, and pharmaceutical compositions for use in such therapy.
- -
-
-
- INHIBITION OF RAF KINASE USING QUINOLYL, ISOQUINOLYL OR PYRIDYL UREAS
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This invention relates to a group of quinolyl, isoquinolyl and pyridyl ureas, their the use in treating raf mediated diseases, and pharmaceutical compositions which contain these ureas for use in such therapy.
- -
-
Page/Page column 8
(2010/11/29)
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- Anti-cancer compounds
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The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like.
- -
-
-
- Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor.
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Inhibitors of the MAP kinase p38 provide a novel approach for the treatment of osteoporosis, inflammatory disorders, and cancer. We have identified N-(3-tert-butyl-1-methyl-5-pyrazolyl)-N'-(4-(4-pyridinylmethyl)phenyl)urea as a potent and selective p38 ki
- Dumas, Jacques,Hatoum-Mokdad, Holia,Sibley, Robert N,Smith, Roger A,Scott, William J,Khire, Uday,Lee, Wendy,Wood, Jill,Wolanin, Donald,Cooley, Jeffrey,Bankston, Donald,Redman, Aniko M,Schoenleber, Robert,Caringal, Yolanda,Gunn, David,Romero, Romulo,Osterhout, Martin,Paulsen, Holger,Housley, Timothy J,Wilhelm, Scott M,Pirro, John,Chien, Du-Shieng,Ranges, Gerald E,Shrikhande, Alka,Muzsi, Andrew,Bortolon, Elizabeth,Wakefield, Jean,Gianpaolo Ostravage, Cynthia,Bhargava, Ajay,Chau, Thuy
-
p. 1559 - 1562
(2007/10/03)
-
- Piperidinylmethyloxazolidinones
-
The invention relates to novel piperidinylmethyloxazolidin-2-one derivatives of the formula I STR1 in which R1 and R2 in each case independently of one another are unsubstituted or mono- to disubstituted phenyl radicals whose substit
- -
-
-
- Studies on the Insecticidal Activities of Some New N-Benzoyl-N'-Arylureas
-
This paper reports the synthesis and the insecticidal activities of some N-benzoyl-N'-arylureas 4-arylsubstituted with alkylated or halogenated aroyl moieties. The compounds, tested against some representative insect species, displayed very high activity against Aedes aegypti, especially the halosubstituted derivatives. None of the newly synthesized compounds showed genotoxic activity in the Bacillus subtilis rec-assay and in the Salmonella-microsome test.
- Carmellino, Maria L.,Pagani, Giuseppe,Pregnolato, Massimo,Terreni, Marco,Caprioli, Vincenzo,Zani, Franca
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p. 227 - 236
(2007/10/03)
-
- Ligand-to-Ligand charge-transfer photochemistry
-
The photochemistry and photophysics are reported for a unique series of complexes of the type fac-(bpy)-ReI(CO)3 -(α-AA), where bpy=2,2′-bipyridine and α-AA is a "reactive donor ligand" that incorporates an α-amino alcohol functional
- Wang, Yinsheng,Hauser, Brian T.,Rooney, Michael M.,Burton, Richard D.,Schanze, Kirk S.
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p. 5675 - 5683
(2007/10/02)
-
- Flexible N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine analogues: Synthesis and monoamine oxidase catalyzed bioactivation
-
Eighteen analogues of N-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) were synthesized and evaluated as substrates of monoamine oxidase. In general, the flexible analogues, characterized by the presence of a methylene (or ethylene) bridge between the aryl/heteroaryl and tetrahydropyridyl moieties, were better substrates of the enzyme than the conformationally restricted MPTP. It is suggested that the increased oxidative activity of these flexible analogues reflects enhanced binding due to the ability of the C-4-aryl/heteroaryl substituent to gain access to a hydrophobic pocket within the substrate binding site.
- Efange,Michelson,Remmel,Boudreau,Dutta,Freshler
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p. 3133 - 3138
(2007/10/02)
-
