- ISOXAZOLINE DERIVATIVES AND THEIR USES IN AGRICULTURE RELATED APPLICATION
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The present invention provides isoxazoline derivatives and uses thereof in agriculture; in particular, the present invention provides a compound having formula (I), or a stereoisomer, an N-oxide or a salt thereof, preparation methods thereof, and compositions containing these compounds and uses thereof in agriculture, particularly uses as herbicide active ingredients for controlling unwanted plants; wherein R1, R2, R3, R4, n, R5, R6 and Hy are as described in the invention.
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Paragraph 00331
(2019/04/26)
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- Bioavailability Studies and in vitro Profiling of the Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitor UCPH-102
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Although the selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor UCPH-101 has become a standard pharmacological tool compound for in vitro and ex vivo studies in the EAAT research field, its inability to penetrate the blood-brain barrier makes it unsuitable for in vivo studies. In the present study, per os (p.o.) administration (40 mg kg-1) of the closely related analogue UCPH-102 in rats yielded respective plasma and brain concentrations of 10.5 and 6.67 μm after 1 h. Three analogue series were designed and synthesized to improve the bioavailability profile of UCPH-102, but none displayed substantially improved properties in this respect. In vitro profiling of UCPH-102 (10 μm) at 51 central nervous system targets in radioligand binding assays strongly suggests that the compound is completely selective for EAAT1. Finally, in a rodent locomotor model, p.o. administration of UCPH-102 (20 mg kg-1) did not induce acute effects or any visible changes in behavior. EAAT1 inhibition beyond the BBB: In the present study, oral administration (40 mg kg-1) of the selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor UCPH-102 in rats yielded respective plasma and brain concentrations of 10.5 and 6.67 μm after 1 h. In vitro profiling of UCPH-102 (10 μm) at 51 central nervous system targets in radioligand binding assays strongly suggests that the compound is fully selective for EAAT1.
- Haym, Isabell,Huynh, Tri H. V.,Hansen, Stinne W.,Pedersen, Martin H. F.,Ruiz, Josep A.,Erichsen, Mette N.,Gynther, Mikko,Bj?rn-Yoshimoto, Walden E.,Abrahamsen, Bjarke,Bastlund, Jesper F.,Bundgaard, Christoffer,Eriksen, Anette L.,Jensen, Anders A.,Bunch, Lennart
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p. 403 - 419
(2016/03/01)
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- Acid Catalyzed Direct-Amidation-Dehydrocyclization of 2-Hydroxy-acetophenones to Benzoxazoles by a One-Pot Sustainable Synthesis
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A series of 2-methyl-benzoxazoles have been synthesized starting from 2-hydroxy-acetophenones via a one-pot three steps reaction. Hydroxylamonium salt has been used as amidation agent. The reaction occurs with different anions, but the best results is achieved with hydroxylamonium hydrchloride. Despite the number of consecutive stages, the reaction is highly selective. Mild reaction conditions and various solvents can be used, but trifluoroacetic acid is the preferred. Almost, complete recovery of the trifluoroacetic acid can be achieved by vacuum distillation. The role of trifluoroacetic acid, as well as, of the hydroxylamonium salt suggests a cooperative effect leading to high selective formation of 2-methyl-benzoxazoles. Graphical Abstract: One-pot TFA catalyzed synthesis of benzoxazoles starting from 2-hydroxyacetophenones. (Chemical Equation Presented).
- Rancan, Elia,Aric, Fabio,Quartarone, Giuseppe,Ronchin, Lucio,Vavasori, Andrea
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p. 939 - 946
(2015/08/06)
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- Benzisoxazole 2-oxides as novel UV absorbers and photooxidation inhibitors
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Compounds with strong absorptions in the ultraviolet (UV) region of the spectrum, particularly the UVA and UVB, have seen much interest as UV screeners or absorbers in a wide variety of commercial products. A series of benzisoxazole 2-oxides have been synthesized and characterized by UV-vis spectroscopy. A number of derivatives have been shown to posses moderate to strong molar absorption coefficients in the UVB range (ca. 300 nm), the strongest being those derived from benzophenones. Three other derivatives containing additional electron withdrawing groups showed strong molar absorption coefficients in the UVA (ca. 340 nm). Solvent effects on the parent derivatives show changes in the molar absorption coefficients with little changes in the λmax values. Preliminary studies of these compounds as potential additives to prevent photooxidation of polystyrene showed considerable inhibition of polymer degradation with the parent unsubstituted benzisoxazole 2-oxide compounds being the most effective. Copyright 2013 John Wiley & Sons, Ltd. A series of benzisoxazole 2-oxides have been shown to posses moderate to strong molar absorption coefficients in the UVB range (ca. 300 nm) and three others with strong absorptions on the UVA (ca. 340 nm). Solvent effects of the parent derivatives show changes in the molar absorption coefficients with little changes in the λmax values. Preliminary studies of these compounds as potential additives to prevent photooxidation of polystyrene showed considerable inhibition of polymer degradation. Copyright
- Kociolek, Martin George,Casbohm, Jerry S.
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p. 863 - 867
(2013/10/01)
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- Synthesis of 1,2-benzisoxazole 2-oxides
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(Chemical Equation Presented) A series of 2-hydroxyaryl ketoximes were converted to the corresponding 1,2- benzisoxazole 2-oxides by treatment with iodobenzene diacetate (in acetic acid or methanol) or N-chlorosuccinimide in water. Both methods gave moderate to excellent yields for a variety of substituted oximes under mild conditions within short reaction times. The latter method has the advantages of an aqueous solvent and lack of halogenated organic by-products. Copyright Taylor & Francis Group, LLC.
- Kociolek, Martin G.,Hoermann, Olivia
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body text
p. 2632 - 2638
(2012/08/08)
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- Microwave-assisted efficient one-step synthesis of amides from ketones and benzoxazoles from (2-hydroxyaryl) ketones with acetohydroxamic acid using sulfuric acid as the catalyst
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Efficient one-step method for the synthesis of amides directly from ketones and benzoxazoles from (2-hydroxyaryl) ketones by the reaction of acetohydroxamic acid using sulfuric acid as catalyst was described.
- Madabhushi, Sridhar,Chinthala, Narsaiah,Vangipuram, Venkata Sairam,Godala, Kondal Reddy,Jillella, Raveendra,Mallu, Kishore Kumar Reddy,Beeram, China Ramanaiah
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experimental part
p. 6103 - 6107
(2011/11/30)
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