- Group 4 metal complexes containing the salalen ligands: Synthesis, structural characterization and studies on the ROP of cyclic esters
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The synthesis of homoleptic salalen ligand supported group 4 complexes and their applications in the ring-opening polymerization (ROP) of ε-caprolactone (?-CL) and lactide (LA) are described. All these complexes of type M(L)2 (LH = (E)-N-(2-(3,
- Chakraborty, Debashis,Rajashekhar, Bijja,Mandal, Mrinmay,Ramkumar, Venkatachalam
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Read Online
- Synthesis of Structurally Diverse Benzotriazoles via Rapid Diazotization and Intramolecular Cyclization of 1,2-Aryldiamines
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An operationally simple method has been developed for the preparation of N-unsubstituted benzotriazoles by diazotization and intramolecular cyclization of a wide range of 1,2-aryldiamines under mild conditions, using a polymer-supported nitrite reagent and p-tosic acid. The functional group tolerance of this approach was further demonstrated with effective activation and cyclization of N-alkyl, -aryl, and -acyl ortho-aminoanilines leading to the synthesis of N1-substituted benzotriazoles. The synthetic utility of this one-pot heterocyclization process was exemplified with the preparation of a number of biologically and medicinally important benzotriazole scaffolds, including an α-amino acid analogue.
- Faggyas, Réka J.,Sloan, Nikki L.,Buijs, Ned,Sutherland, Andrew
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supporting information
p. 5344 - 5353
(2019/05/21)
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- Fe-based metal-organic frameworks for the synthesis of N-arylsulfonamides via the reactions of sodium arylsulfinates or arylsulfonyl chlorides with nitroarenes in water
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A newly developed chemoselective reaction of sodium arylsulfinates or arylsulfonyl chlorides with nitroarenes has been disclosed. The chemistry, in which non-toxic water and recyclable iron-based metal-organic frameworks are employed as the solvent and catalyst, respectively, provides an efficient approach for the generation of N-arylsulfonamides, which are widely present in biologically active compounds and drugs, rendering this methodology attractive to both synthetic and medicinal chemistry.
- Li, Xinxin,Chen, Fei,Lu, Guo-Ping
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supporting information
p. 4226 - 4230
(2018/10/26)
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- Amide type organic nitrogen ligand compound and synthesis method thereof
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The invention is claimed to protect an N-(2-(bis(2-hydroxyl-2-methyl propyl)amido)phenyl) amide type organic nitrogen ligand compound and a preparing method thereof. The method is simple and feasibleand is supplementation and development in the field of o
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Paragraph 0019; 0020; 0021
(2018/06/28)
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- A novel serine racemase inhibitor suppresses neuronal over-activation in vivo
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Serine racemase (SRR) is an enzyme that produces D-serine from L-serine. D-Serine acts as an endogenous coagonist of NMDA-type glutamate receptors (NMDARs), which regulate many physiological functions. Over-activation of NMDARs induces excitotoxicity, which is observed in many neurodegenerative disorders and epilepsy states. In our previous works on the generation of SRR gene knockout (Srr-KO) mice and its protective effects against NMDA- and Aβ peptide-induced neurodegeneration, we hypothesized that the regulation of NMDARs’ over-activation by inhibition of SRR activity is one such therapeutic strategy to combat these disease states. In the previous study, we performed in silico screening to identify four compounds with inhibitory activities against recombinant SRR. Here, we synthesized 21 derivatives of candidate 1, one of four hit compounds, and performed screening by in vitro evaluations. The derivative 13J showed a significantly lower IC50 value in vitro, and suppressed neuronal over-activation in vivo.
- Mori, Hisashi,Wada, Ryogo,Takahara, Satoyuki,Horino, Yoshikazu,Izumi, Hironori,Ishimoto, Tetsuya,Yoshida, Tomoyuki,Mizuguchi, Mineyuki,Obita, Takayuki,Gouda, Hiroaki,Hirono, Shuichi,Toyooka, Naoki
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p. 3736 - 3745
(2017/06/13)
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- BENZENE SULFONAMIDE-BASED INHIBITORS OF SPHINGOSINE KINASE
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A novel class of sphingosine kinase (SK) inhibitor compounds are disclosed which are useful in the treatment of cancer and other proliferative cell conditions. The compounds are benzene sulfonamides with a chemical structure according to formula (I).
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Paragraph 00137
(2016/03/13)
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- SERINE RACEMASE INHIBITOR
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A novel serine racemase inhibitor exhibits sufficient activity and specificity. The serine racemase inhibitor includes one or more compounds selected from compounds respectively represented by the following general formulas [MM_1], [DR_1], [DR'_1], [LW_1], and [ED_1] as an active ingredient.
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Paragraph 0186 - 0190
(2014/12/12)
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- A one-pot synthetic strategy for construction of the dibenzodiazepine skeleton via a transition metal-free process
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A one-pot transition metal-free methodology for constructing pharmacologically active dibenzodiazepine derivatives was developed. Fluoro-, bromo- and nitro-substituted aryl aldehydes were applied to this reaction efficiently. This journal is the Partner Organisations 2014.
- Fang, Shuai,Niu, Xiaoyi,Zhang, Zeyuan,Sun, Yan,Si, Xiaomeng,Shan, Cuicui,Wei, Lei,Xu, Aiqing,Feng, Lei,Ma, Chen
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p. 6895 - 6900
(2014/09/30)
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- Palladium-catalyzed intramolecular sulfonamidation/oxidation of imines: Access to multifunctional benzimidazoles
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O-Sulfonamidophenylimines undergo intramolecular sulfonamidation/oxidation to produce 1,2-disubstituted benzimidazoles upon treatment with palladium(II) chloride/(diacetoxyiodo)benzene and potassium carbonate at room temperature. The substituent scope at
- Fu, Shaomin,Jiang, Huanfeng,Deng, Yuanfu,Zeng, Wei
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experimental part
p. 2795 - 2804
(2011/12/01)
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- Highly enantioselective aldol reactions using N-arylprolinamides with enhanced acidity and double H-bonding potential
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We have designed and synthesized N-arylprolinamides 7-10 with a potential to involve in the binding of electrophilic aldehydes via two N-H?O hydrogen bonds for application in organocatalytic aldol reactions. The catalyst 10 is shown to afford aldol produc
- Saha, Satyajit,Moorthy, Jarugu Narasimha
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supporting information; experimental part
p. 912 - 916
(2010/05/03)
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- Catalysis by design: Wide-bite-angle diphosphines by assembly of ditopic ligands for selective rhodium-catalyzed hydroformylation
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The assembly makes the bite! Ditopic ligands comprising an anionic N-O or N-N moiety (shown in blue and gray) and a phosphine moiety (orange) can be assembled with hard metals such as zinc(II) (green) to form bidentate phosphine ligands. This approach led to a rhodium catalysts for the selective hydroformylation of 1-octene with linear-to-branched ratios up to 21:1 and rates comparable to covalently bound wide-bite-angle diphosphine ligands. (Figure Presented).
- Rivillo, David,Gulyas, Henrik,Benet-Buchholz, Jordi,Escudero-Adan, Eduardo C.,Freixa, Zoraida,Van Leeuwen, Piet W. N. M.
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p. 7247 - 7250
(2008/09/17)
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- Direct asymmetric aldol reaction catalyzed by simple prolinamide phenols
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Simple prolinamides 1a-f were synthesized, and their catalytic effects on the direct asymmetric aldol reactions in organic solvents and in water were evaluated. Prolinamide phenols 1a-d were found to be effective catalysts for the reaction of aromatic ald
- Fu, Yu-Qin,Li, Zai-Chun,Ding, Li-Na,Tao, Jing-Chao,Zhang, Sheng-Hong,Tang, Ming-Sheng
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p. 3351 - 3357
(2007/10/03)
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- Metal complexes of a novel achiral symmetric pentadentate ligand - Crystal structures of monohelical zinc(II) and cadmium(II) complexes
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By both electrochemical synthesis and a traditional chemical procedure the interaction of the pentadentate ligand 2,6-bis{1-[2-(tosylamino)phenylimino]ethyl}pyridine (H2DAPATs), with MnII, FeII, CoII, NiII
- Pedrido, Rosa,Bermejo, Manuel R.,Garcia-Deibe, Ana M.,Gonzalez-Noya, Ana M.,Maneiro, Marcelino,Vazquez, Miguel
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p. 3193 - 3200
(2007/10/03)
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- Studies on aroylation of o-phenylenediamine and subsequent reactions with electrophiles
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Condensation of o-phenylenediamine 1 with benzoyl chloride in pyridine results in the formation of dibenzoyl derivative 2 irrespective of the molar ratios employed. However, the reaction of 1 with arylsulphonyl chlorides gives a mono 3 and diarylsulphonyl
- Dubey,Kulkarni, Subhash M.,Vinod Kumar
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p. 1305 - 1309
(2007/10/03)
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- Tautomerism and stereodynamics of indophenols, amidines, their derivatives, and analogs: XIV. New methods of synthesis of spiro-fused quinoxalines
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A new procedure was proposed for synthesis of quinoxaline derivatives by N-alkylation of 2,6-ditert-butyl-4-(o-R-sulfonylaminophenylimino)-2,5-cyclohexadienones and subsequent intramolecular spirocyclization. A necessary condition for the reaction to occu
- Kurbatov,Vikrishchuk,Simakov,Kuznetsov,Zhdanov,Olekhnovich
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p. 950 - 955
(2007/10/03)
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- Decisive role of Al3+ cation in the electrodetosylation of N, N'-bis- (o-tosylaminophenyl) propanediamide to N, N'-bis-(o-aminophenyl) propanediamide
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The reductive electrodetosylation of N, N'-bis-(o-tosylaminophenyl) propanediamide was performed in an undivided cell fitted with a sacrificial aluminum anode, at constant current and at room temperature. The completion of the reduction process was favour
- Lu
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p. 16721 - 16730
(2007/10/03)
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- Transition Metal Complexes Containing a Tosyl Group
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Physicochemical properties of nickel(II), cobalt(II), and copper(II) chelates based on the o-tosyl-aminophenyl derivative of β-aminovinyl phenyl ketone have been studied by ESR and IR spectroscopy, and magnetochemical measurements. Quantum-chemical (CNDO/
- Bondarenko
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p. 584 - 589
(2007/10/03)
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- Photolysis of p-Toluenesulfonyl Azide and Its Charge-Transfer Complex with Aniline
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Photolysis of p-toluenesulfonyl azide (1) in p-xylene and cyclohexane gives primarily the products derived from insertion of (p-tolylsulfonyl)nitrene into the solvent.For p-xylene, an unstable intermediate product is formed which decomposes in the dark at room temperature to give both the ring-insertion product and the corresponding p-toluenesulfonamide (2).Photolysis of the ground-state charge-transfer complex between p-toluenesulfonyl azide and aniline gives six products, the major product being the sulfonyl hydrazide 7.Furthermore, formation of the insertion product by reaction with the solvent provides evidence for production of (p-tolylsulfonyl)nitrene from the excited charge-transfer complex.
- Hoyle, C. E.,Lenox, R. S.,Christie, P. A.,Shoemaker, R. A.
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p. 2056 - 2061
(2007/10/02)
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- MODELS OF FOLATE COENZYMES-VII SYNTHESIS AND CARBON TRANSFER REACTIONS OF N5,N10-METHENYL AND N5,N10-METHYLENETETRAHYDROFOLATE MODELS
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Carboxylate esters react with 1,2-diaminoethanes to yield imidazolines, which upon consecutive reaction with acetic anhydride or tosyl chloride and methyl iodide give imidazolinium salts that serve as models of N5,N10-(CH+)-tetrahydrofolate (THF) coenzymes (7a,b and 18a,b).Reduction of the latter salts with sodium borohydride or reaction with anions (R-) give the corresponding 5,10--THF models.Mono- and bifunctional nucleophiles react with 18a,b to yield carbon-transfer products. 6-Alkylamino-1,3-dimethyluracils react with 1-tosyl-3,4,4-trimethylimidazolidine (the reduction product of 18b), in the presence of acetic acid, to form carbon-transfer products via a mechanism which bears close analogy to the mechanism of action of thymidylate synthetase.
- Bieraeugel, H.,Plemp, R.,Hiemstra, H. C.,Pandit, U. K.
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p. 3971 - 3980
(2007/10/02)
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- Diphenylamino and indolyl substituted pyromellitides
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This invention relates to 3,7-bis(disubstituted aminophenyl- or indolyl)-3,7-bis(diphenylamino)pyromellitides, 3,5-bis(disubstituted aminophenyl- or indolyl)-3,5-bis(diphenylamino)pyromellitides and mixtures thereof useful as color formers, particularly in carbonless duplicating and thermal marking systems, which are prepared by the interaction of 2,5-bis(disubstituted aminophenyl- or indolyl)carbonyl-1,4-benzenedicarboxylic acids or 2,4-bis(disubstituted aminophenyl- or indolyl)carbonyl-1,5-benzenedicarboxylic acids and mixtures thereof with diphenylamines.
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