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Facile oxidation of electron-poor benzo[b]thiophenes to the corresponding sulfones with an aqueous solution of H2O2 and P 2O5

A facile oxidation for the clean conversion of benzo[b]thiophenes to their corresponding sulfones is described employing an aqueous solution of H 2O2 and P2O5; the solution can be prepared and stored on a multi-gram scale with a shelf-life of up to two weeks.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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PHARMACEUTICAL COMPOUNDS

This invention relates to compounds of formula (I) where R1 to R12,–W–V–,–X–Y–, m and n have the values defined in claim 1, their preparation and use as pharmaceuticals.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Electrophilic Aromatic Substitution. Part 33. Partial Rate Factors for Protiodetritiation of Benzothiophen; the Resonance-dependent Reactivity of the Ring Positions

Rate coefficients for detriation of benzothiophen, specifically labelled with tritium at each position, have been measured in anhydrous trifluoroacetic acid, and, for <2-3H>benzothiophen, in a range of trifluoroacetic acid-acetic acid mixtures, all at 70 deg C.The dependence of rate upon acidity is consistent with the effect of hydrogen bonding between sulphur and trifluoroacetic acid, as found previously for other sulphur-containing heterocycles.Partial rate factors, corrected for the effect of hydrogen bonding are (positions in parentheses): 8.84 * 105 (2); 1.18 * 106 (3); 360 (4); 13200 (5); 16200 (6); and 26.2 (7); the corresponding ?+ values are -0.68, -0.695, -0.29, -0.47, -0.48, and -0.16.The positional reactivity order is the same as found in pyrolysis of 1-arylethyl acetates, and solvolysis of 1-arylethyl chlorides, but the ?+ values are more negative due to the greater demand for resonance stabilization of the transition states in hydrogen exchange.Comparison of the 2- : 3-isomer ratios in various substitutions leads to the unexpected conclusion that substitution at the 2-position is subject to steric effects, probably due to the proximity of the sulphur d-orbitals.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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FUNCTIONALLY SELECTIVE ALPHA2C ADRENORECEPTOR AGONISTS

In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of y2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the y2C adrenergic receptors using such compounds or pharmaceutical compositions.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Enantioselective Radical Ring-Opening Cyanation of Oxime Esters by Dual Photoredox and Copper Catalysis

Catalytic enantioselective chemical reactions involving highly reactive radical species remain largely unexplored. We report herein for the first time a novel enantioselective radical ring-opening cyanation of redox-active oxime esters by dual photoreodox and copper catalysis. This mild protocol shows good functional group tolerance and broad substrate scope, producing a wide range of optically active alkyl dinitriles with high yields and excellent enantioselectivities, which are difficult to access traditionally.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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1. 3 – Disubstituted ketenes compound and use thereof (by machine translation)

The invention relates to a kind of formula (I) of the structure shown in Figure 1, 3 – disubstituted compound ketenes and its application. The compounds mainly activated PPAR alpha, to the PPPA delta and PPPA gamma have agonistic activity. Can be used for the treatment of PPAR regulating abnormal various diseases associated, such as non-alcoholic fatty liver disease particularly in the treatment of non-alcoholic hepatitis, also used for the treatment of diabetes, obesity, fibrotic diseases, cardiovascular disease (including heart failure and atherosclerosis and the like), kidney disease (including chronic renal disease and renal failure and the like), cerebral degenerative diseases (including Alzheimer’s disease and the like) such as the potential of the, has great application value. (by machine translation)

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Oxalic Diamides and tert-Butoxide: Two Types of Ligands Enabling Practical Access to Alkyl Aryl Ethers via Cu-Catalyzed Coupling Reaction

A robust and practical protocol for preparing alkyl aryl ethers has been developed, which relies on using two types of ligands to promote Cu-catalyzed alkoxylation of (hetero)aryl halides. The reaction scope is very general for a variety of coupling partners, particularly for challenging secondary alcohols and (hetero)aryl chlorides. In case of coupling with aryl chlorides and bromides, two oxalic diamides serve as the powerful ligands. The tert-butoxide is first demonstrated as a ligand for Cu-catalyzed coupling reaction, leading to alkoxylation of aryl iodides complete at room temperature. Additionally, a number of carbohydrate derivatives are applicable for this coupling reaction, affording the corresponding carbohydrate-aryl ethers in 29-98% yields.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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N-Arylation of Carbamates through Photosensitized Nickel Catalysis

A highly efficient method of visible light mediated Ni(II)-catalyzed photoredox N-arylation of Cbz-amines/Boc-amines with aryl electrophiles at room temperature is reported. The methodology provides a common access to a wide variety of N-aromatic and N-heteroaromatic carbamate products that find use in the synthesis of several biologically active molecules and provides a distinct advantage over traditional palladium-catalyzed Buchwald reaction.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Practical Direct alpha-Arylation of Cyclopentanones by Palladium/Enamine Cooperative Catalysis

Direct arylation of cyclopentanones has been a long-standing challenge because of competitive self-aldol condensation and multiple arylations. Reported herein is a direct mono-alpha-C-H arylation of cyclopentanones with aryl bromides which is enabled by palladium/amine cooperative catalysis. This method is scalable and chemoselective with broad functional-group tolerance. Application to controlled sequential arylation of cyclopentanones has been also demonstrated. Be direct: A direct alpha-C-H arylation of normal cyclopentanones with aryl bromides, enabled by palladium/amine cooperative catalysis, features an exceptionally high selectivity for monoarylation, use of readily available starting materials, good scalability, and broad functional-group tolerance.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Hole transport materials including OLED applications

The composition described here comprises at least one hole-transporting compound, wherein the hole-transporting compound comprises a core covalently bonded to at least two arylamine groups, wherein the arylamine group optionally comprises one or more intractability groups. The composition can provide good film formation and stability when coated onto hole injection layers. Solution processing of hole transporting layers of OLEDs can be achieved with the composition described here. Good mobility can be achieved.

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Reference£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem