- Synthesis, properties, and remarkable 2 D self-assembly at the liquid/solid interface of a series of triskele-shaped 5,11,17-triazatrinaphthylenes (TrisK)
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A series of 5,11,17-triazatrinaphthylene (TrisK) derivatives, large disk-like π-conjugated molecules with C3h symmetry, has been synthesised by following an optimised synthetic pathway. The synthesis was performed by a four-step protocol based
- Bertrand, Helene,Guillot, Regis,Teulade-Fichou, Marie-Paule,Fichou, Denis
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Read Online
- Preparation technology of 6-hydroxy-bentazone
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The invention discloses a preparation technology of 6-hydroxy-3-isopropyl-1H-benzo[c][1,2,6]thiadiazine-4(3H)-keto-2,2-dioxide. The preparation technology includes subjecting 5-chloro-2-nitrobenzoic acid serving as a raw material to hydrolysis reaction an
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Paragraph 0019-0020; 0035-0036; 0051-0052; 0067-0068
(2017/08/28)
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- HETEROCYCLIC COMPOUNDS, PROCESS FOR PREPARATION OF THE SAME AND USE THEREOF
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The present invention provides a heterocyclic compound represented by the formula (I), its stereoisomers, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and their use in preparing a medicament for the prevention and/or treatment of central nervous system disease.
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Paragraph 0330; 0331; 0332
(2017/07/15)
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- METHOD FOR SPECIFIC CLEAVAGE OF C Alpha-C BOND AND SIDE CHAIN OF PROTEIN AND PEPTIDE, AND METHOD FOR DETERMINING AMINO ACID SEQUENCE
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The present invention provides a method for specifically cleaving a Cα-C bond of a peptide backbone and/or a side chain of a protein and a peptide, and a method for determining amino acid sequences of protein and peptide. A method for specifically cleaving a Cα-C bond of a peptide backbone and/or a side chain bond of a protein or a peptide, comprising irradiating a protein or a peptide with laser light in the presence of at least one hydroxynitrobenzoic acid selected from the group consisting of 3-hydroxy-2-nitrobenzoic acid, 4-hydroxy-3-nitrobenzoic acid, 5-hydroxy-2-nitrobenzoic acid, 3-hydroxy-5-nitrobenzoic acid, and 4-hydroxy-2-nitrobenzoic acid. A method for determining an amino acid sequence of a protein or a peptide, comprising irradiating a protein or a peptide with laser light in the presence of the above specific hydroxynitrobenzoic acid to specifically cleave a Cα-C bond of a peptide backbone and/or a side chain bond, and analyzing generated fragment ions by mass spectrometry.
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- A practical approach for regioselective mono-nitration of phenols under mild conditions
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Cu(NO3)2.3H2O was demonstrated to be an efficient, regioselective and inexpensive nitrating reagent for the synthesis of mono-nitro substituted phenolic compounds. 12 examples of different phenols were examined. Good yields (67-90%) have been achieved. ARKAT-USA, Inc.
- Chen, Ling-Yan,Liu, Tao,Zhou, Xiaokun,Sun, Zhihua
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- Supramolecular oxidation of anilines using hydrogen peroxide as stoichiometric oxidant
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6A,6D-Di-O-(propan-2-on-1,3-diyl) α-cyclodextrin-6A,6D-dicarboxylate (2α) and 6A,6D-di-O-(propan-2-on-1,3-diyl) β-cyclodextrin-6A,6D-dicarboxylate (2β) were found to catalyze the oxidation of aromatic amines in the presence of hydrogen peroxide. The products were the corresponding nitro compounds or in some cases azo-, azoxy-, or other dimerization products. The catalysis was found to follow enzyme kinetics giving a rate increase (kcat/kuncat) of up to 1100 in the best case. Copyright
- Marinescu, Lavinia,Molbach, Merete,Rousseau, Cyril,Bols, Mikael
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p. 17578 - 17579
(2007/10/03)
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- Nitrophenol derivatives oxidized by cerium(IV) ammonium nitrate (CAN) and their cytotoxicity
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Oxidation of a series of phenols with cerium(IV) ammonium nitrate (CAN) in acetonitrile undermild conditions yields the mixture of corresponding nitrophenols. In the cases of methylphenols and hydroxy-carboxylic acids, the steric effect may reduce the nitration reaction. Compounds 3 a and 4b showed selective activities to Hep 3B and Hep G2 cancer cell lines, respectively. Compound 2c showed selective activities to Hep G2 and MDA-MB-231 cancer cell lines. Further more, com pound 10b showed selective activities to Hep G2, Hep 3B, MCF-7 and MDA-MB-231 cancer cell lines.
- Pan, Wen-Bin,Wei, Li-Mei,Wei, Li-Lan,Wu, Chin-Chung,Chang, Fang-Rong,Wu, Yang-Chang
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p. 581 - 588
(2007/10/03)
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- 1H-IMIDAZO[4,5-c]QUINOLINE DERIVATIVES IN THE TREATMENT OF PROTEIN KINASE DEPENDENT DISEASES
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The invention relates to the use of imidazoquinolines and salts thereof in the treatment of protein kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases, imidazoquinolines for use in the treatment of protein kinase dependent diseases, a method of treatment against said diseases, comprising administering the imidazoloquinolines to a warm-blooded animal, especially a human, pharmaceutical preparations comprising an imidazoquinoline, especially for the treatment of a protein kinase dependent disease, novel imidazoquinolines, and a process for the preparation of the novel imidazoquinolines.
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Page/Page column 63
(2008/06/13)
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- An expedient synthesis of 7-O-functionalised pyrrolo[2,1-c][1,4]benzodiazepine-5,11-diones
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An efficient synthetic route to 7-hydroxypyrrolo[2,1-c][1,4]benzodiazepine-5,11-dione, an important potential ligand for the DNA minor groove, has been developed. Simultaneous reduction of nitro and hydrogenolysis of the O-benzyl in N-(5-benzyloxy-2-nitro
- Madani, Hadi,Thompson, Andrew S,Threadgill, Michael D
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p. 8107 - 8111
(2007/10/03)
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- Photochemical transformation of acifluorfen under laboratory and natural conditions
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Acifluorfen was irradiated in pure water at various excitation wavelengths and pH values. Numerous photoproducts were obtained which were identified by [1H]NMR and /or HPLC-MS/MS. The main reaction pathways were photo-decarboxylation, photo-cleavage of the ether bonding with formation of phenolic compounds, photo-dechlorination and photo-Claisen type rearrangement. Decarboxylation was observed in acidic and neutral media whereas cleavage of the ether bonding dominated in basic media. The photo-Claisen type rearrangement only occurred on excitation at short wavelengths. The quantum yield of photolysis was significantly lower at 313nm (6.1 × 10-5) than at 254nm (2.0 × 10-3). The photoreactivity of acifluorfen was then studied in conditions approaching environmental conditions. Acifluorfen was dissolved in pure water, in water containing humic substances or in a natural water, and exposed to solar light in June at Clermont-Ferrand (latitude 46°N). In pure water, the half-life was estimated at 10 days and photo-decarboxylation accounted for 30% of the conversion. The presence of humic substances (10mg litre-1) did not affect the rate of photo-transformation. However, the half-life of acifluorfen dissolved in the natural water was only 6.8 days.
- Vialaton, Delphine,Baglio, Daniela,Paya-Perez, Ana,Richard, Claire
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p. 372 - 379
(2007/10/03)
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- Photochemical degradation of acifluorfen in aqueous solution
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To elucidate the photochemical behavior of diphenyl ether herbicides in superficial waters, the photodegradation of acifluorfen, 5-[2-chloro-4-(trifluoromethyl)phenoxy]-2-nitrobenzoic acid (CAS Registry No. 50594-66-6), was studied in water and acetonitrile. All experiments were carried out under laboratory conditions using a solar simulator (xenon arc) or jacket Pyrex reaction cell equipped with a 125 W high-pressure mercury lamp. The calculated polychromatic quantum efficiencies (Φsolvent) of acifluorfen in different solvents are as follows (units are degraded molecules photon-1): Φwater = 10-4, Φacetronitile = 10-4, Φmethanol = 10-4, and Φhexane = 10-2. The results obtained in this work are in good agreement with the literature value of monochromatic quantum yield. HPLC-MS analysis (APCI and ESI in positive and negative modes) was used to identify acifluorfen photoproducts. These results suggest that the photodegradation of acifluorfen proceeds via a number of reaction pathways: (1) decarboxylation, (2) dehalogenation, (3) substitution of chlorine group by hydroxyl or hydrogen groups, and (4) cleavage of ether linkage, giving phenols. Photorearrangement products were studied by other investigators. No such products were observed. In addition, it was found that the trifluoro functional group on acifluorfen was not affected by any transformation, and no products of a nitro group reduction were found.
- Vulliet,Emmelin,Scrano,Bufo,Chovelon,Meallier,Grenier-Loustalot
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p. 4795 - 4800
(2007/10/03)
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- Substituted 11-oxo-11H-pyrido[2,1-b]quinazolines and method of inhibiting allergic reactions with them
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Pyrido[2,1-b]quinazolines of the formulas STR1 wherein R1, R1 ', R2, R2 ', R3, R3 ', R4 and R10 are as hereinafter set forth, and processes for the preparation thereof
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- 1-Heterocyclic alkyl-1,2,3,4-tetrahydroquinazolinones and analgesic intermediates thereof
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1-Heterocyclic alkyl-1,2,3,4-tetrahydroquinazolinones, acid addition salts thereof, and intermediate compounds having analgesic properties. A representative quinazolinone compound is 1-[2-(1-phenyl-4-piperazinyl)-ethyl]-2-phenyl-1,2,3,4-tetrahydro-4-quinazolinone. A representative analgesic intermediate is 2-[2-(4-[1-phenyl]piperazinyl)ethylamino] bezamide.
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- 1-Heterocyclic alkyl-1,2,3,4-tetrahydroquinazolinones and analgesic intermediates thereof
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1-heterocyclic alkyl-1,2,3,4-tetrahydroquinazolinones, acid addition salts thereof, and intermediate compounds having analgesic properties. A representative quinazolinone compound is 1-[2-(1-phenyl-4-piperazinyl)-ethyl]-2-phenyl-1,2,3,4-tetrahydro-4-quinazolinone. A representative analgesic intermediate is 2-[2-(4-[1-phenyl]piperazinyl)ethylamino]benzamide.
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