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PROCESS FOR THE PREPARATION OF BREXPIPRAZOLE

Processes for preparation of Brexpiprazole, intermediates used during preparation, and polymorphs of Brexpiprazole are provided.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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A process for the synthesis of the preparation method of the paipai zuo according to matching (by machine translation)

The invention provides a method for synthesizing according to the matching of the paipai zuo preparation method, specific steps are as follows: to 4 – nitrobenzene [b] thiophene as raw materials hydrogenation reaction synthetic intermediate compound (II), in order to 7 – hydroxy – 1H – quinoline – 2 – ketone as a raw material 1st step reaction to synthesize compound (III), 2nd step to obtain the intermediate compound (IV). Then the intermediate compound (II) and (IV) intermediate compound condensation to obtain the target compound (I), namely according to the paipai zuo. The invention the whole synthetic route of the reaction raw materials, simple operation, low operation cost, environmental protection, and the various steps in the yield of the reaction is high, it is very suitable for industrial production, has a very high industrial application value. (by machine translation)

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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This new pharmaceutical use (6-1, 6-dihydro-2-yl) amide derivative, as the inhibitor of this preparation and AKT (PKB) phosphoenzyme (by machine translation)

The invention relates to the novel materials of formula (I), wherein each of the substituents R, R1, R2, R3, R4 and R5 is as defined herein. The materials are useful as inhibitors of AKT(PKB) phosphorylation.

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Enhanced durability of linker-containing carbon nanotube functionalized via diazonium reaction

We present the fabrication of highly durable catalysts with the functionalized carbon nanotube (CNT) via diazonium chemistry for polymer electrolyte membrane fuel cell (PEMFC). The functionalization of the CNT with the thiolphenyl groups by diazonium coupling reaction was shown to enhance the dispersion of Pt nanoparticles with narrow size distribution deposited on the CNT surfaces as well as their electrochemical stability. The electrochemical analysis demonstrates that the Pt/functionalized CNT show higher electrochemical durability and catalytic activity than the Pt/unmodified CNT. The enhanced electrochemical performance of the Pt/functionalized CNT is attributed to the uniform distribution of Pt nanoparticles with smaller size and the strong interaction between Pt and the functionalized CNT support through the formation of Pt-sulfur bonding. This study shows that this simple functionalization of CNT by the in situ grafting of the thiolphenyl groups as the linker onto the surface is an effective way to fabricate a highly durable Pt catalyst for PEMFC, thus providing a design guide of the functionalized CNT support catalyst with a great potential as a PEMFC catalyst.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. The reactant in an enzyme-catalyzed reaction is called a substrate. Safety of Benzo[b]thiophen-4-amine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 17402-83-4, Name is Benzo[b]thiophen-4-amine, molecular formula is C8H7NS

Towards the development of an in vivo chemical probe for cyclin G associated kinase (GAK)

SGC-GAK-1 (1) is a potent, selective, cell-active chemical probe for cyclin G-associated kinase (GAK). However, 1 was rapidly metabolized in mouse liver microsomes by cytochrome P450-mediated oxidation, displaying rapid clearance in liver microsomes and in mice, which limited its utility in in vivo studies. Chemical modifications of 1 that improved metabolic stability, generally resulted in decreased GAK potency. The best analog in terms of GAK activity in cells was 6-bromo-N-(1H-indazol-6-yl)quinolin-4-amine (35) (IC50 = 1.4 muM), showing improved stability in liver microsomes while still maintaining a narrow spectrum activity across the kinome. As an alternative to scaold modifications we also explored the use of the broad-spectrum cytochrome P450 inhibitor 1-aminobenzotriazole (ABT) to decrease intrinsic clearance of aminoquinoline GAK inhibitors. Taken together, these approaches point towards the development of an in vivo chemical probe for the dark kinase GAK.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Ipiprazole derivative and preparation method thereof (by machine translation)

The invention provides a piripiprazole derivative and a preparation method, wherein the chemical structural formula of the epiprazole derivative is expressed by a chemical structural formula. The epiprazole derivative is composed of epiconazole, (HCHO). m N – hydroxymethyl according to the first basic catalyst is prepared; and then N – hydroxymethyl-piripiprazole and an alkylformylchloride compound are reacted under second basic catalyst to prepare. The half-life of the epiprazole derivative is prolonged, the drug delivery frequency can be reduced; and the epiprazole derivative prepared by the preparation method is low in impurity, and low in cost. (by machine translation)

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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1,2,4-TRIAZINE-6-CARBOXAMIDE DERIVATIVE

The present invention provides a compound represented by the following general formula (I) or a salt thereof which has a Syk inhibitory effect (in the formula R1 represents a hydrogen atom or an optionally Ra-substituted C1-C6 alkyl group; A represents a hydrogen atom, an optionally Ra-substituted C1-C8 alkyl group, an optionally Ra-substituted C2-C6 alkenyl group, an optionally Ra-substituted C2-C6 alkynyl group, an optionally Rb-substituted C3-C10 cycloalkyl group, an optionally Rb-substituted C6-C14 aromatic hydrocarbon group, an optionally Rb-substituted 4- to 10-membered unsaturated heterocyclic group, or an optionally Rb-substituted 4-to 10-membered saturated heterocyclic group, or optionally forms a 4- to 10-membered unsaturated heterocyclic ring or a 4- to 10-membered saturated heterocyclic ring together with R1 and the nitrogen atom bonded thereto; R2 represents a hydrogen atom or an optionally Ra-substituted C1-C6 alkyl group; and B represents an optionally Rc-substituted unsaturated heterocyclic group).

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

 

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A method for preparing brexpiprazole (by machine translation)

The invention discloses a kind of type (1) a compound represented by the method for preparing brexpiprazole, particularly in 4–aminobenzene and [b] thiophene as the starting material for synthesizing ethylene, to avoid heavy metal palladium-catalyzed reaction, synthesis step and impurities is reduced, reducing the cost of the preparation method. (by machine translation)

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Smiles rearrangement for the synthesis of 5-amino-substituted [1]benzothieno[2,3-b]pyridine

The Smiles rearrangement was successfully applied to 4-hydroxybenzo[b]thiophene furnishing a facile entry to the 4-amino derivative. The rearrangement was extended to 5-methoxy-4-methoxycarbonyl[1]benzothieno[2,3-b]pyridine obtained via aza-Wittig/electrocyclization reaction of novel N-(4-methoxybenzothiophen-2-yl)iminomethyldiphenylphosphorane with methyl trans-4-oxo-2-pentenoate. The preparation of a novel 5-amino-4-methoxycarbonyl[1]benzothieno[2,3-b]pyridine, which is of interest as a potential secondary peptide structure mimic, was successfully achieved.

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

 

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Chemical Compound, Pharmaceutical Composition Thereof, and Use and Application Thereof

Provided are a pyrimidinyl amino compound having protein kinase inhibitor activity, and a pharmaceutical composition containing said compound; also provided are a use and application of said compound. What is provided is selected from a group consisting of the compound represented by formula (I), a stereoisomer thereof, a tautomer thereof, a pharmacologically acceptable salt thereof, a solvate thereof, and a prodrug thereof. The described compound has good inhibitory activity against the JAK family of kinases and the SYK family of kinases, and therefore may serve as a JAK inhibitor and SYK inhibitor, and is effective in use for the prevention or treatment of diseases related to the JAK and SYK families of kinases.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem