The Absolute Best Science Experiment for Methyl benzo[b]thiophene-2-carboxylate

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Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model

FLT3 mutation is among the most common genetic mutations in acute myeloid leukemia (AML), which is also related with poor overall survival and refractory in AML patients. Recently, FLT3 inhibitors have been approved for AML therapy. Herein, a series of new compounds with pyrazole amine scaffold was discovered, which showed potent inhibitory activity against FLT3-ITD and significant selectivity against both FLT3-ITD and AML cells expressing FLT3-ITD. Compound 46, possessing the most promising cellular activity, blocked the autophosphorylation of FLT3 pathway in MV4-11 cell line. Furthermore, the apoptosis and downregulation of P-STAT5 were also observed in tumor cells extracted from the MV4-11 cell xenografts model upon compound 46 treatment. Compound 46 was also metabolically stable in vitro and suppressed tumor growth significantly in MV4-11 xenografts model in vivo. Compound 46 showed no toxicity to the viscera of mice and caused no decrease in body weight of mice. In conclusion, the results of this study could provide valuable insights into discovery of new FLT3 inhibitors, and compound 46 was worthy of further development as potential drug candidate to treat AML.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

New explortion of 63675-74-1

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Benzothiophene compounds, intermediates, compositions, and methods

A method for alleviating the symptoms of post-menopausal syndrome comprising administering to a woman in need thereof an effective amount of a compound of formula I wherein R1a is –H or –OR7a in which R7a is –H or a hydroxy protecting group; R2a is –H, halo, or –OR8a in which R8a is –H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and Z is –O– or –S–; or a pharmaceutically acceptable salt thereof, and further comprising administering to said woman an effective amount of progestin.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Final Thoughts on Chemistry for 5-Aminobenzothiophene

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A synthetic method of the compound aromatic amines (by machine translation)

The invention discloses a method for synthesizing aromatic amine compound, characterized in that in accordance with the following two kinds of methods in any method for carrying out: method a: will have the general formula (I) of the alkyl aromatic compound having the general formula (II) with the nitrogen containing compound mixed, oxidizing agent and organic solvent in the presence of reaction under the condition of having the general formula (III) of the aromatic amine compound; the second method: will have the general formula (I ‘) of the aromatic alcohol derivatives having the general formula (II) with the nitrogen containing compound mixed, in the acid additive and the presence of organic solvent prepared through the reaction of the formula (III) of the aromatic amine compound. The invention of the first use of the bulk of the alkyl aromatic compound or aromatic alcohol derivatives as raw materials, under the action of the non-metal catalytic, produced by the reaction of aromatic amine compound, compared with the traditional synthetic method with high yield, condition is simple, less waste emissions, does not need metal involved in, the reaction apparatus is simple, easy to industrial production and the like, therefore, has a wide application. (by machine translation)

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Simple exploration of 4-Chlorobenzo[b]thiophene

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Reference of 66490-33-3, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 66490-33-3, Name is 4-Chlorobenzo[b]thiophene, molecular formula is C8H5ClS. In a Article£¬once mentioned of 66490-33-3

Solvent-free mechanochemical Buchwald-Hartwig amination of aryl chlorides without inert gas protection

A solvent-free Buchwald-Hartwig amination had been developed under high-speed ball-milling conditions, which afforded the desired products with moderate to high yields. The addition of sodium sulfate was found to be crucial for improving both the performance and the reproducibility. Comparative solvent-free stirring experiments implicated the importance of mechanical interaction for the transformation, and the inert gas was proved to be unnecessary for this amination.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Some scientific research about 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

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Intermediates and a process for preparing benzo[B]thiophenes

The instant invention provides intermediates and processes for the preparation of compounds of formula IV STR1 wherein: n is 0, 1, or 2; R is hydrogen or C1 -C4 alkyl; X1 is hydrogen, cyano, 4-hydroxybenzoyl, 4-halobenzoyl, or 4-(C1 -C4 alkoxy)benzoyl; Y is NR4 R5, 4-hydroxyphenyl, or 4-(C1 -C4 alkoxy)phenyl; and R4 and R5 are independently hydrogen or C1 -C4 alkyl.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Awesome Chemistry Experiments For Methyl 3-aminobenzo[b]thiophene-2-carboxylate

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BENZOFURO- AND BENZOTHIENOPYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR

Benzofuro-and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.

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

 

New explortion of 5-Bromobenzothiophene

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Carboxylation of Aromatic and Aliphatic Bromides and Triflates with CO2 by Dual Visible-Light?Nickel Catalysis

We report the efficient carboxylation of bromides and triflates with K2CO3 as the source of CO2 in the presence of an organic photocatalyst in combination with a nickel complex under visible light irradiation at room temperature. The reaction is compatible with a variety of functional groups and has been successfully applied to the synthesis and derivatization of biologically active molecules. In particular, the carboxylation of unactivated cyclic alkyl bromides proceeded well with our protocol, thus extending the scope of this transformation. Spectroscopic and spectroelectrochemical investigations indicated the generation of a Ni0 species as a catalytic reactive intermediate.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Extended knowledge of 1196-19-6

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Related Products of 1196-19-6, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 1196-19-6, 3-(Bromomethyl)benzo[b]thiophene, introducing its new discovery.

4-Substituted D-glutamic acid analogues: The first potent inhibitors of glutamate racemase (MurI) enzyme with antibacterial activity

The first potent inhibitors of glutamate racemase (MurI) enzyme that show whole cell antibacterial activity are described. Optically pure 4-substituted D-glutamic acid analogues with (2R,4S) stereochemistry and bearing aryl-, heteroaryl-, cinnamyl-, or biaryl-methyl substituents represent a novel class of glutamate racemase inhibitors. Exploration of the D-Glu core led to the identification of lead compounds (-)-8 and 10. 2-Naphthylmethyl derivative 10 was found to be a potent competitive inhibitor of glutamate racemase activity (Ki = 16 nM, circular dichroism assay; IC50 = 0.1 mug/mL high-performance liquid chromatography (HPLC) assay). Thorough structure-activity relationship (SAR) studies led to benzothienyl derivatives such as 69 and 74 with increased potency (IC50 = 0.036 and 0.01 mug/mL, respectively, HPLC assay). These compounds showed potent whole cell antibacterial activity against S. pneumoniae PN-R6, and good correlation with the enzyme assay. Compounds 69, 74 and biaryl derivative 52 showed efficacy in an in vivo murine thigh infection model against Streptococcus pneumoniae. Data described herein suggest that glutamate racemase may be a viable target for developing new antibacterial agents.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

A new application about 2,3-Dibromobenzo[b]thiophene

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Application of 6287-82-7, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 6287-82-7, molcular formula is C8H4Br2S, introducing its new discovery.

BENZOTHIOPHENE DERIVATIVE AND USE THEREOF IN ORGANIC ELECTROLUMINESCENT FIELD

The present invention refers to type (I) as relates to compounds to be represented by, state and used in the R 1 and R 2 in an independently a substituted or unsubstituted C 4-C 30amine it will be biting of, a substituted or unsubstituted C 4-C 40 for dozing, , a substituted or unsubstituted C 4-C 40 of benzo mote five pen or a substituted or unsubstituted C 4-C 40 of benzo […] and, selected from a, L is the bridging group, single joined, C 4-C 40 of substituted arylamine, C 4-C 40 carbazole-substituted, C 4-C 40 substituted benzothiophene, oxygen atoms, nitrogen atoms or sulfur and one selected from nuclear reactor, R 3-R 10 independently H atoms, C 1-C 20 aliphatic straight or branched chain hydrocarbon groups or C 6-C 888000081488 8 selected from aromatic group or two groups is connected adjacent the upper end the ring form a derivatives […] , m, integer of at 0-3 graphical object is selected from the n, 3 the m+n less than or equal is greater than 0. The present invention refers to in addition said types of compound use in organic electroluminescence device protects the material exhibits hole-transporting by performing a polishing process in particular OLED, hole injection material or organic light-emitting material protection a main composition. (by machine translation)

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Brief introduction of Benzo[b]thiophene-6-carbaldehyde

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Syntheses and analytical characterizations of novel (2-aminopropyl)benzo[b]thiophene (APBT) based stimulants

Two groups of amphetamine-like drugs with psychostimulant properties that were first developed during the course of scientific studies and later emerged as new psychoactive substances (NPS) are based on the (2-aminopropyl)indole (API) and (2-aminopropyl)benzofuran (APB) structural scaffolds. However, sulfur-based analogs with a benzo[b]thiophene structure (resulting in (2-aminopropyl)benzo[b]thiophene (APBT) derivatives) have received little attention. In the present investigation, all six racemic APBT positional isomers were synthesized in an effort to understand their structure?activity relationships relative to API- and APB-based drugs. One lesson learned from the NPS phenomenon is that one cannot exclude the appearance of such substances on the market. Therefore, an in-depth analytical characterization was performed, including various single- and tandem mass spectrometry (MS) and ionization platforms coupled to gas chromatography (GC) and liquid chromatography (LC), nuclear magnetic resonance spectroscopy (NMR), and solid phase and GC condensed phase infrared spectroscopy (GC-sIR). Various derivatizations have also been explored; it was found that all six APBT isomers could be differentiated during GC analysis after derivatization with heptafluorobutyric anhydride and ethyl chloroformate (or heptafluorobutyric anhydride and acetic anhydride) under non-routine conditions. Discriminating analytical features can also be derived from NMR, GC-EI/CI- single- and tandem mass spectrometry, LC (pentafluorophenyl stationary phase), and various infrared spectroscopy approaches (including GC-sIR). Availability of detailed analytical data obtained from these novel APBT-type stimulants may be useful to researchers and scientists in cases where forensic and clinical investigations are warranted.

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