16440-97-4Relevant academic research and scientific papers
The identification of indacaterol as an ultralong-acting inhaled β2-adrenoceptor agonist
Baur, Fran?ois,Beattie, David,Beer, David,Bentley, David,Bradley, Michelle,Bruce, Ian,Charlton, Steven J.,Cuenoud, Bernard,Ernst, Roland,Fairhurst, Robin A.,Faller, Bernard,Farr, David,Keller, Thomas,Fozard, John R.,Fullerton, Joe,Garman, Sheila,Hatto, Julia,Hayden, Claire,He, Handan,Howes, Colin,Janus, Diana,Jiang, Zhengjin,Lewis, Christine,Loeuillet-Ritzler, Frederique,Moser, Heinz,Reilly, John,Steward, Alan,Sykes, David,Tedaldi, Lauren,Trifilieff, Alexandre,Tweed, Morris,Watson, Simon,Wissler, Elke,Wyss, Daniel
, p. 3675 - 3684 (2010)
Following a lipophilicity-based hypothesis, an 8-hydroxyquinolinone 2-aminoindan derived series of β2-adrenoceptor agonists have been prepared and evaluated for their potential as inhaled ultralong-acting bronchodilators. Determination of their activities at the human β2-adrenoceptor receptor showed symmetrical substitution of the 2-aminoindan moiety at the 5- and 6-positions delivered the targeted intermediate potency and intrinsic-efficacy profiles relative to a series of clinical reference β2-adrenoceptor agonists. Further assessment with an in vitro superfused electrically stimulated guinea-pig tracheal-strip assay established the onset and duration of action time courses, which could be rationalized by considering the lipophilicity, potency, and intrinsic efficacy of the compounds. From these studies the 5,6-diethylindan analogue indacaterol 1c was shown to possess a unique profile of combining a rapid onset of action with a long duration of action. Further in vivo profiling of 1c supported the long duration of action and a wide therapeutic index following administration to the lung, which led to the compound being selected as a development candidate.
Silver-Catalyzed Carbon Dioxide Fixation on Alkynylindenes
Chuang, Po-Yao,Okumura, Akira,Saito, Kodai,Yamada, Tohru
, (2020)
The synthesis of polycyclic indene derivatives via silver-catalyzed carbon dioxide fixation on 2-alkynylindene derivatives was achieved by nucleophilic addition of the indenyl anion to carbon dioxide involving carbon-carbon bond formation and subsequent intramolecular cyclization to the alkyne part activated by a silver catalyst. This cascade process could be applied to various substrates to obtain the corresponding products in high yields. The endo/exo selectivity of the cyclization could be controlled by the steric or electronic effect of the substituents on the substrates, and 6-endo-selective cyclization was realized to afford α-pyrone-fused indenes.
TRANSITION METAL COMPOUND AND METHOD FOR PRODUCING OLEFIN POLYMER
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Paragraph 0072, (2018/11/27)
PROBLEM TO BE SOLVED: To provide a transition metal compound catalyst that makes it possible to synthesize an olefin polymer that is soft and has improved catalytic activity and reduced stereoregularity, and a method for producing an olefin polymer. SOLUTION: The present invention provides a compound represented by formula (IV) (X is a σ-binding or π-binding ligand; Y is a Lewis base; Y may be crosslinked to other Y and X; q is an integer of 1-5 and [(valence of M)-2]; r is an integer of 0-3; R1 and R2 independently represent H or halogen, alkyl or the like; R3-R10 are alkyl groups. M is metal elements of groups 3-10 or lanthanoid series in the periodic table; A1-A4 independently represent a crosslinking group composed of group 14 (C, Si, Ge, Sn)). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
METALLOCENE COMPLEX AND OLEFIN POLYMERIZATION METHOD
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Paragraph 0147; 0254, (2015/11/03)
Provided are a metallocene complex that facilitates copolymerization of olefin monomers including propylene at a higher uptake rate of comonomers, i.e., ethylene and α-olefin, manufacture of a rubber component having a higher molecular weight, and manufac
METALLOCENE COMPLEX AND METHOD FOR PRODUCING OLEFIN POLYMER
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Paragraph 0130, (2016/10/07)
PROBLEM TO BE SOLVED: To provide a metallocene complex which, in homopolymerization of propylene, can produce homopolypropylene having a high melting point, and a method for producing an olefin polymer using the same. SOLUTION: Provided is a metallocene complex crosslinked by Si, such as dichlorosilacyclobutylenebis[2-(5-methyl-2-furyl)-4-phenyl-1,5,6,7-tetrahydro-s-indacen-1-yl]zirconium and dichlorosilacyclopentylenebis[2-(5-methyl-2-furyl)-4-phenyl-1,5,6,7-tetrahydro-s-indacen-1-yl]zirconium. Also provided is a catalyst for polymerizing an olefin such as propylene, comprising the complex, a compound which forms an ion pair by reacting with the complex or an ion-exchanging phyllosilicate, and an organoaluminum compound. COPYRIGHT: (C)2016,JPOandINPIT
Regioselectivity of acid-catalyzed cyclization of 1-(3,4-dialkylaryl)-3- chloropropan-1-ones to indanones. Comparison of experimental data and results of computer simulation
Ivchenko,Nifant'Ev,Ustynyuk,Ezerskii
experimental part, p. 929 - 935 (2010/10/04)
The acid-catalyzed cyclization of 1-(3,4-dialkylaryl)-3-chloropropan-1-ones to dialkyl-indanones via the intermediate formation of (3,4-dialkylaryl) propenones was studied. This reaction affords isomeric products: 5,6-dialkylindan-1-ones and 4,5-dialkylin
LIGANDS AND CATALYSTS FOR PRODUCING ELASTOMERIC PROPYLENE POLYMERS
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, (2008/06/13)
A ligand useful to form a metallocene olefin polymerization catalyst comprises:wherein at least R3 and R4 are substituents having at least a bulk of a t-butyl group and, optionally, wherein R1 or R2 may be a bulky substituent group.
Aromatic Spiranes XX [1]: Syntheses of Dimethylsubstituted 2-Carboxymethyl-indan-1-ones and Benzylchlorides as Synthones for Syntheses of di- to tetramethylsubstituted Spirobiindandiones
Neudeck
, p. 185 - 200 (2007/10/03)
The isomeric dimethyl methylbenzoates 5, obtained from the bromides via Grignard reactions with dimethylcarbonate, were reduced with LiAlH4 to the hydroxymethyl derivatives 6. The latter were then transformed both to the benzylchlorides 7 (with SOCl2) and to the aldehydes 8 (with pyridinium chlorochromate). Knoevenagel-Doebner reaction of 8 afforded the acrylic acids 9 which (after hydrogenation to 11) were cyclized to the desired indanones 12 with polyphosphoric acid. On the other hand, 12c and 12e were prepared from dimethyl 3-chloropropiophenone (14) by warming with sulfuric acid. After NaH-catalyzed reaction with dimethylcarbonate, the indanones 12 gave the ketoesters 15 which then could be hydrogenated to the indanes 16. All reactions proceeded with satisfactory to excellent yields (60-90%).
