22422-23-7

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.

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

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

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.

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

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