- Photoredox Activation of Formate Salts: Hydrocarboxylation of Alkenes via Carboxyl Group Transfer
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A photoredox activation mode of formate salts for carboxylation was developed. Using a formate salt as the reductant, carbonyl source, and hydrogen atom transfer reagent, a wide range of alkenes can be converted into acid products via a carboxyl group tra
- Huang, Yan,Hou, Jing,Zhan, Le-Wu,Zhang, Qian,Tang, Wan-Ying,Li, Bin-Dong
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p. 15004 - 15012
(2021/12/14)
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- Synthesis method of succinic acid derivative or 3 -arylpropionic acid (by machine translation)
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The invention discloses a synthesis method of a succinic acid derivative or 3 -arylpropionic acid, which comprises the following steps: adding a base in a drying reaction tube and CO removing CO. 2 The reaction is carried out under the irradiation of visible light, the reaction is carried out under visible light irradiation, and then separation and purification are carried out to obtain the butanedioic acid derivative or 3 -arylpropionic acid product; the base comprises sodium tert-butoxide, potassium tert-butoxide, lithium tert-butyl alcohol and 4 - potassium carbonate; and the reaction substrate comprises an acrylate compound or an aryl vinyl compound. CO can be induced by visible light. 2 The scheme provided by the invention is mild in reaction condition and wide in reaction 3 - substrate selectivity, and the reaction substrate is wide in selectivity, the raw materials are cheap and easily available, and the method has a good industrial application prospect. (by machine translation)
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Paragraph 0101-0114; 0115; 0125
(2020/10/30)
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- Method for selective reduction α, β - unsaturated carbonyl compound carbon-carbon double bond (by machine translation)
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The invention discloses a method for selectively reducing carbon-carbon double bonds in α and β - unsaturated carbonyl compounds, which comprises the following steps of adding α, β - unsaturated carbonyl compounds shown in formula (I) in an electrolysis system and reducing α and β - unsaturated carbonyl compounds with carbonyl-conjugated carbon-carbon double bonds through an electrochemical cathodic reduction reaction. Compared with the reported method, the method disclosed by the invention does not use a metal catalyst and an external oxidant; and the reaction raw material and the electrolyte are low in price, nontoxic and tasteless, simple and convenient in post-treatment. (by machine translation)
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Paragraph 0051-0054
(2020/06/17)
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- Site-Selective, Remote sp3 C?H Carboxylation Enabled by the Merger of Photoredox and Nickel Catalysis
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A photoinduced carboxylation of alkyl halides with CO2 at remote sp3 C?H sites enabled by the merger of photoredox and Ni catalysis is described. This protocol features a predictable reactivity and site selectivity that can be modulated by the ligand backbone. Preliminary studies reinforce a rationale based on a dynamic displacement of the catalyst throughout the alkyl side chain.
- Sahoo, Basudev,Bellotti, Peter,Juliá-Hernández, Francisco,Meng, Qing-Yuan,Crespi, Stefano,K?nig, Burkhard,Martin, Ruben
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supporting information
p. 9001 - 9005
(2019/06/24)
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- Regioselectivity inversion tuned by iron(iii) salts in palladium-catalyzed carbonylations
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Impactful regioselectivity control is crucial for cost-effective chemical synthesis. By using cheap and abundant iron(iii) salts, the hydroxycarbonylations of both aromatic and aliphatic alkenes were significantly enhanced in both reactivity and selectivity (iso/n or n/iso up to >99:1). Moreover, Pd-catalyzed carbonylation selectivity can be switched from branched to linear by using different Fe(iii) salts. In addition, similar results were obtained for the carbonylation of secondary alcohols.
- Huang, Zijun,Cheng, Yazhe,Chen, Xipeng,Wang, Hui-Fang,Du, Chen-Xia,Li, Yuehui
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supporting information
p. 3967 - 3970
(2018/04/23)
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- A Ligand-Directed Catalytic Regioselective Hydrocarboxylation of Aryl Olefins with Pd and Formic Acid
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An effective Pd-catalyzed hydrocarboxylation of aryl olefins with Ac2O and formic acid is described. A variety of 2- and 3-arylpropanoic acids can be regioselectively formed by the judicious choice of ligand without the use of toxic CO gas.
- Liu, Wei,Ren, Wenlong,Li, Jingfu,Shi, Yuan,Chang, Wenju,Shi, Yian
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supporting information
p. 1748 - 1751
(2017/04/11)
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- Synthetic Applications and Mechanistic Studies of the Hydroxide-Mediated Cleavage of Carbon-Carbon Bonds in Ketones
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The hydroxide-mediated cleavage of ketones into alkanes and carboxylic acids has been reinvestigated and the substrate scope extended to benzyl carbonyl compounds. The transformation is performed with a 0.05 M ketone solution in refluxing xylene in the presence of 10 equiv of potassium hydroxide. The reaction constitutes a straightforward protocol for the synthesis of certain phenyl-substituted carboxylic acids from 2-phenylcycloalkanones. The mechanism was investigated by kinetic experiments which indicated a first order reaction in hydroxide and a full negative charge in the rate-determining step. The studies were complemented by a theoretical investigation where two possible pathways were characterized by DFT/M06-2X. The calculations showed that the scission takes place by nucleophilic attack of hydroxide on the ketone followed by fragmentation of the resulting oxyanion into the carboxylic acid and a benzyl anion.
- Mazziotta, Andrea,Makarov, Ilya S.,Fristrup, Peter,Madsen, Robert
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p. 5890 - 5897
(2017/06/07)
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- Pd nanoparticles on reverse phase silica gel as recyclable catalyst for Suzuki-Miyaura cross coupling reaction and hydrogenation in water
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Two catalytic systems, consisting of palladium nanoparticles supported by reverse phase amino functionalized silica are utilized as catalysts for Suzuki-Miyaura reaction and hydrogenation in water. The catalysts were developed by modifying silica into bidentate ligands, using either 2-pyridinecarboxaldehyde or 2,2′-bipyridine-4,4′-dicarboxylic acid. The synthesized catalysts showed quantitative reaction yields and recyclability with negligible leaching of Pd nanoparticles. Various characterization techniques including XPS, ICP-MS, SEM, BET, XRD, TEM, 1H- and 13C- NMR are used to verify the efficiency of the catalysts.
- Shabbir, Saira,Lee, Sinyoung,Lim, Minkyung,Lee, Heejin,Ko, Hyeji,Lee, Youngbok,Rhee, Hakjune
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p. 296 - 304
(2017/07/12)
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- Minimizing Aryloxy Elimination in RhI-Catalyzed Asymmetric Hydrogenation of β-Aryloxyacrylic Acids using a Mixed-Ligand Strategy
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The first example of efficient asymmetric hydrogenation of challenging β-aryloxyacrylic acids was realized using a RhI-complex based on the heterocombination of a readily available chiral monodentate secondary phosphine oxide (SPO) and an achiral monodentate phosphine ligand as the catalyst. Excellent enantioselectivities (92->99% ee) were achieved for a wide variety of chiral β-aryloxypropionic acids with minor aryloxy elimination in most cases. The resultant products were readily transformed into biologically active compounds through simple synthetic manipulations.
- Li, Yang,Wang, Zheng,Ding, Kuiling
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p. 16387 - 16390
(2015/11/09)
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- Compositions comprising an aryl pyrazole and a substituted imidazole, methods and uses thereof
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This invention relates to compositions for combating parasites in animals, comprising 1-arylpyrazole compounds in combination with substituted imidazole compounds. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infestation in an animal comprising administering the compositions of the invention to an animal in need thereof.
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- COMPOSITIONS COMPRISING AN ARYL PYRAZOLE AND A SUBSTITUTED IMIDAZOLE, METHODS AND USES THEREOF
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This invention relates to compositions for combating parasites in animals, comprising 1-arylpyrazole compounds in combination with substituted imidazole compounds. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infestation in an animal comprising administering the compositions of the invention to an animal in need thereof.
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- Rhodium(I)-catalyzed 1,4-addition of arylboronic acids to acrylic acid in water: One-step preparation of 3-arylpropionic acids
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A practical method for the one-step preparation of 3-arylpropionic acids through rhodium-catalyzed 1,4-addition of arylboronic acids to acrylic acid is reported. The method is applicable to a broad scope of aryl boronic acids and displays a wide functional group tolerance operating in water as the optimal reaction medium. Georg Thieme Verlag Stuttgart · New York.
- Vautravers, Nicolas R.,Breit, Bernhard
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supporting information; experimental part
p. 2517 - 2520
(2011/11/12)
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- Pd nanoparticles dispersed on solid supports: Synthesis, characterization and catalytic activity on selective hydrogenation of olefins in aqueous media
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Two types of Pd nanoparticle catalysts were prepared having 2-4 nm particle size using silica gel and porous polymer beads as solid supports. 2-Pyridinecarboxaldehyde ligand was anchored on commercially available 3-aminopropyl-functionalized silica gel followed by Pd metal dispersion. Bead-shaped cross-linked poly(4-vinylpyridine-co-styrene) gel was prepared by an emulsifier-free emulsion polymerization of 4-vinylpyridine, styrene and divinylbenzene in the presence of ammonium persulfate and subsequently dispersing the Pd metal on the synthesized polymer. These catalysts were characterized by SEM, TEM and ICP techiniques with respect to appearance, size and possible leaching out, respectively. Furthermore, the reactivity of these catalysts was tested on hydrogenation of various α,β-unsaturated carbonyl compounds using aqueous solvent under a hydrogen balloon (1 atm). The results showed that the Pd dispersed on silica was a more efficient catalyst than Pd dispersed on polymer and the former could be recycled more than 10 times without considerable loss in activity. Copyright
- Lim, Minkyung,De Castro, Kathlia A.,Oh, Seungchan,Lee, Kangsuk,Chang, Young-Wook,Kim, Hokun,Rhee, Hakjune
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scheme or table
p. 1 - 8
(2011/09/14)
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- THERAPEUTIC FLUOROETHYLCYANO GUANIDINES
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Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
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Page/Page column 17
(2008/12/04)
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- 1,4-Cyclohexadiene with Pd/C as a rapid, safe transfer hydrogenation system with microwave heating
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A method for the rapid, safe hydrogenation of alkenes and deprotection of benzyl ethers and carboxybenzyl amides is described using catalytic transfer hydrogenation under microwave heating conditions. Commonly available Pd/C catalyst is extremely effective with 1,4-cyclohexadiene as the hydrogen transfer source. In general, the reactions are complete within five minutes at 100 °C.
- Quinn, John F.,Razzano, Dana A.,Golden, Kathryn C.,Gregg, Brian T.
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scheme or table
p. 6137 - 6140
(2009/04/05)
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- Indirect ortho functionalization of substituted toluenes through ortho olefination of N,N-dimethylbenzylamines tuned by the acidity of reaction conditions
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Highly regioselective olefination of substituted N,N-dimethylbenzylamines was developed by tuning the acidity of reaction conditions based on analysis of their features. The ortho-functionalized N,N-dimethylbenzylamines were further transformed into 3-(2′
- Cai, Guixin,Fu, Ye,Li, Yizhou,Wan, Xiaobing,Shi, Zhangjie
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p. 7666 - 7673
(2008/02/09)
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- Direct synthesis of 3-arylpropionic acids by tetraphosphine/palladium catalysed Heck reactions of aryl halides with acrolein ethylene acetal
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Through the use of [PdCl(C3H5)]2/Cis,cis, cis-1,2,3,4-tetrakis(diphenylphosphinomethyl)cyclopentane as a catalyst, a range of aryl bromides undergoes Heck reaction with acrolein ethylene acetal. With this acetal, the selective formation of 3-arylpropionic acids/esters was observed. The functional group tolerance on the aryl halide is remarkable; substituents such as fluoro, methyl, methoxy, acetyl, formyl, benzoyl, nitro or nitrile are tolerated. Furthermore, this catalyst can be used at low loading, even for reactions of sterically hindered aryl bromides. Graphical Abstract.
- Lemhadri, Mhamed,Doucet, Henri,Santelli, Maurice
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p. 11533 - 11540
(2007/10/03)
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- Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues
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The in vitro evaluation of a series of saturated prostaglandins revealed that compounds with omega chin aromatic rings retain nanomolar potency for the human prostaglandin F receptor (hFP receptor), exemplified by compound 8. In contrast, the double bonds are required for activity in the series with an acyclic omega chain as in PGF(2α). (C) 2000 Published by Elsevier Science Ltd.
- DeLong, Mitchell A.,Amburgey, Jack,Taylor, Cynthia,Wos, John A.,Soper, David L.,Wang, Yili,Hicks, Renee
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p. 1519 - 1522
(2007/10/03)
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- Medetomidine analogs as α2-adrenergic ligands. 3. Synthesis and biological evaluation of a new series of medetomidine analogs and their potential binding interactions with α2-adrenoceptors involving a 'methyl pocket'
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The synthesis and the biological evaluation of a new series of medetomidine analogs are reported. The substitution pattern at the phenyl ring of the tetralin analogs had a distinct influence on the α2- adrenoceptor binding affinity. 4-Methylindan analog 6 was the most potent α2-adrenoceptor binding ligand among these 4-substituted imidazoles, and its α2-adrenoceptor selectivity was greater than the 5-methyl tetralin analog 4c. Ligand-pharmacophore and receptor modeling were combined to rationalize α2-adrenoceptor binding data of the imidazole analogs in terms of ligand-receptor interactions. The structure-activity relationships that were apparent from this and previous studies were qualitatively rationalized by the binding site models of the α2-adrenoceptor. The benzylic methyl group of medetomidine or the naphthyl analog 2a was superimposable with the α-methyl group of (-)-α-methylnorepinephrine and fit into the proposed 'methyl pocket' of the α2-adrenoceptor defined by the residues Leu110, Leu169, Phe391, and Thr395.
- Zhang, Xiaoyan,De Los Angeles, Joseph E.,He, Mei-Ying,Dalton, James T.,Shams, Gamal,Lei, Longping,Patil, Popat N.,Feller, Dennis R.,Miller, Duane D.,Hsu, Fu-Lian
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p. 3014 - 3024
(2007/10/03)
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- Substituted dihydroisoquinolinones and related compounds as potentiators of the lethal effects of radiation and certain chemotherapeutic agents; selected compounds, analogs and process
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The invention is selected, novel, and known analogs of isoquinolinones of the formula and pharmaceutically acceptable salts thereof; novel pharmaceutical compositions; and a method for enhancing the lethal effects for tumor cells to treatment having DNA damaging activity such as ionizing radiation or with chemotherapeutic agents.
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- Synthesis of Polycyclic Aromatic Hydrocarbons via a Novel Annelation Method
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A new general synthetic approach to polycyclic aromatic hydrocarbons is described.The method is based on the convenient availability of o-lithioarylamides from regiospecific metalation of N,N-diethylarylamides with alkyllithium-amine reagents.Addition of the o-lithioarylamide to an aryl ketone or aldehyde affords a lactone.Reduction of the latter with zinc and alkali or HI generates the free acid which undergoes cyclization with ZnCl2 and Ac2O and reduction with zinc and alkali or HI to furnish the fully aromatic polyarene.Compounds synthesized via this route include 3-methylcholanthrene, benzanthracene, dibenzanthracene, dibenzanthracene, benzopyrene, and their methyl derivatives.Overall yields are generally good.Competitive enolate anion formation depresses the yield in the initial step in the reactions of enolizable ketones.However, this pathway can be suppressed with substantial improvement in yield through deuterium exchange of the hydrogens α to the carbonyl.The last three steps of the general method can be condensed to only one step through reductive cyclization of the lactone intermediates with hydriodic acid in acetic acid.While tertiary lactones are resistant to HI under these conditions, the corresponding free acids undergo reductive cyclization under similar conditions.
- Harvey, Ronald G.,Cortez, Cecilia,Jacobs, Stephen A.
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p. 2120 - 2125
(2007/10/02)
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- SYNTHESIS OF 3-METHYLCHOLANTHRENE
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A novel synthesis of 3-methylcholanthrene is described which is operationally simpler than the method in current use and is potentially applicable to the synthesis of a wide range of other polycyclic hydrocarbons and their oxidized carcinogenic metabolites.
- Jacobs, Stephen A.,Harvey, Ronald G.
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p. 1093 - 1096
(2007/10/02)
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