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FUSED BICYCLOHETEROCYCLE SUBSTITUTED AZABICYCLIC ALKANE DERIVATIVES

The invention relates to fused bicycloheterocycle substituted azabicyclic alkane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Step-Edge Assisted Direct Linear Alkane Coupling

Direct coupling of alkanes via C?H activation of terminal methyl groups has acquired tremendous interests both scientifically and technically. Herein we present the results of linear alkane-coupling at the step edges of Cu surfaces at modulated temperatures. Combining the observations of scanning tunneling microscopy (STM) with density functional theory plus dispersion (DFT-D) calculations, we elucidate the mechanism of the reaction and demonstrate that the low activation barrier relies on heterogeneous catalysis at the upper step edges, where low-coordinated surface atoms are present. We further reveal the generality of the reaction, so that it can be applied on the step edges of different facets of surfaces.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Modulation of aggregation-induced emission and electroluminescence of silole derivatives by a covalent bonding pattern

The deciphering of structure-property relationships is of high importance to rational design of functional molecules and to explore their potential applications. In this work, a series of silole derivatives substituted with benzo[b]thiophene (BT) at the 2,5-positions of the silole ring are synthesized and characterized. The experimental investigation reveals that the covalent bonding through the 2-position of BT (2-BT) with silole ring allows a better conjugation of the backbone than that achieved though the 5-position of BT (5-BT), and results in totally different emission behaviors. The silole derivatives with 5-BT groups are weakly fluorescent in solutions, but are induced to emit intensely in aggregates, presenting excellent aggregation-induced emission (AIE) characteristics. Those with 2-BT groups can fluoresce more strongly in solutions, but no obvious emission enhancements are found in aggregates, suggesting they are not AIE-active. Theoretical calculations disclose that the good conjugation lowers the rotational motions of BT groups, which enables the molecules to emit more efficiently in solutions. But the well-conjugated planar backbone is prone to form strong intermoelcular interactions in aggregates, which decreases the emission efficiency. Non-doped organic light-emitting diodes (OLEDs) are fabricated by using these siloles as emitters. AIE-active silole derivatives show much better elecroluminescence properties than those without the AIE characterisic, demonstrating the advantage of AIE-active emitters in OLED applications. Stay connected! Connecting benzo[b]thiophene with a silole ring through its 2- or 5-position furnishes silole derivatives with totally different photoluminescence and electroluminescence properties (see figure).

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Ir(III)-Catalyzed Oxidative Annulation of Phenylglyoxylic Acids with Benzo[ b]thiophenes

An Ir(III)-catalyzed oxidative annulation of phenylglyoxylic acids with benzo[b]thiophenes for the construction of benzothieno[3,2-c][2]benzopyranones in one step is disclosed. Three C-H cleavages and C-C/C-O bond formations are involved in this reaction. This protocol features a relatively broad substrate scope, good functional group tolerance, good regioselectivities, mild reaction conditions, and scale-up synthesis.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Direct Carboxylation of Electron-Rich Heteroarenes Promoted by LiO-tBu with CsF and [18]Crown-6

We herein demonstrate that the combination of LiO-tBu, CsF, and [18]crown-6 efficiently promotes the direct C?H carboxylation of electron-rich heteroarenes (benzothiophene, thiophene, benzofuran, and furan derivatives). A variety of functional groups, including methyl, methoxy, halo, cyano, amide, and keto moieties, are compatible with this system. The reaction proceeds via the formation of a tert-butyl carbonate species.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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A facile synthesis of 4-aryl-1,2,3,4-tetrahydroisoquinolines

A facile and versatile palladium catalyzed alpha-arylation between dihydroisoquinolinones and various aryl halides is described. Combined with borane reduction, it provides a convenient way to prepare 4-aryl-1,2,3,4- tetrahydroisoquinolines.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Synthesis of Borinic Acids and Borinate Adducts Using Diisopropylaminoborane

In situ formation of aryl Grignard under Barbier condition and diisopropylaminoborane as boron source allows a complete control of the addition onto the boron electrophile. Analytically pure borinic acid derivatives were produced at the gram scale without column chromatography and isolated as borinates adducts, with ethanolamine or 8-hydroxyquinoline, after workup.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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New squarylium derivative, and organic thin-film solar cell (by machine translation)

[A] without changing the energy level, improving the carrier mobility of a thin film state, and further improve the fill factor (FF) new squarylium derivative of improving energy conversion efficiency. Also, the novel squarylium derivative of donor material and organic thin film solar cell. [Solution] (1) Derivatives represented by the general formula squalirium. (In the general formula (1), R1 And R2 Is, independently, the number of carbon atoms or a branched aliphatic substituents 4, R3 – R6 Is, independently, a hydrogen atom, aliphatic group or aromatic substituents, R3 And R4 , Or, R5 And R6 Each ring may be coupled together to form, X1 X and2 Is, each independently, represent – O – or – S -. )[Drawing] no (by machine translation)

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Benzothiophene – Wikipedia,
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Palladium-Catalyzed Cascade Reductive and Carbonylative Cyclization of Ortho-Iodo-Tethered Methylenecyclopropanes (MCPs) Using N-Formylsaccharin as CO Source

A palladium-catalyzed reductive and carbonylative cyclization of ortho-iodo-tethered methylenecyclopropanes (MCPs) using N-formylsaccharin as CO source has been developed, affording the desired indanone derivatives in moderate to good yields with high regio- and stereoselectivity and good functional group compatibility.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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FUSED HETEROCYCLE DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND MEDICINAL USE THEREOF

The present invention provides fused heterocyclic derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof, or prodrugs thereof, which exhibit an inhibitory activity in human SGLT and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications or obesity, in the formula R1 to R4 represent H, OH, an amino group, etc.; R5 and R6 represent H, OH, a halogen atom, an optionally substituted alkyl group, etc. ; Q represents alkylene, alkenylene, etc.; ring A represents an aryl group or a heteroaryl group; the following ring (R1) represents a group represented by the following ring (R2); G represents a group represented by the following general formula (G-1) or (G-2) (E1 represents H, F or OH; and E2 represents H, F, a methyl group, etc.), and pharmaceutical compositions comprising the same, and pharmaceutical uses thereof.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem