Awesome and Easy Science Experiments about 22913-24-2

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The present invention provides novel transition metal complexes (e.g., complexes of any one of Formulae (C1) to (C25)) that include an amine-N-oxide motif. The invention also provides methods of using these transition metal complexes in preparing N-aryl or N- heteroaryl sulfonimides (e.g., compounds of Formula (I)) and aryl or heteroaryl amines (e.g., compounds of Formula (II)). The inventive methods involve imidation of arenes and heteroarenes (e.g., compounds of Formula (A)) using an imidating agent (e.g., a compound of Formula (B), such as N-fluorobenzenesulfonimide (NFBS or NFSI)) in the presence of a single-electron reductant (e.g., an Ag(I) or Ru(II) salt).

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Awesome and Easy Science Experiments about 4-Chlorobenzo[b]thiophene

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A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT1A receptor antagonism and serotonin reuptake inhibition was discovered. 1-(1H-Indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols exhibited selective and high affinity at the 5-HT1A receptor and serotonin reuptake inhibition at nanomolar concentrations for dual activities.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Final Thoughts on Chemistry for 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

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In this study we extended our studies on heterocyclic antiestrogens to 2-phenylbenzo[b]thiophenes which can be considered as isosteric to the 2- phenylindole system. We synthesized a number of 6-hydroxy-2-(4- hydroxyphenyl)benzo[b]thiophenes with carbamoyl and amino functions in the side chain at carbon-3 and analyzed their biological properties. The binding affinities for the estrogen receptor are mainly influenced by the chain length whereas the hormonal profile depends on the nature of the functional group. From this study 3-[10-(2,2,3,3,4,4,4,-heptafluorobutyl- methylcarbamoyl)decyl]-6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thiophene (6e) emerged as an antiestrogen with all the characteristics of a pure antagonist. It did not stimulate gene expression in HeLa cells cotransfected with the expression vector for the human estrogen receptor HEGO and the luciferase reporter plasmid EREwtc luc nor did it show any estrogenic activity in the mouse uterus weight test. In the latter assay, it completely abrogated the stimulatory effect of estrone. Due to its antiestrogenic potency it strongly inhibited the growth of estrogen-sensitive human MCF-7 breast cancer cells with an IC50 value of 5 nM. These data suggest that an amide function is combination with the fluorination of the terminal carbon atoms is an appropriate modification to abolish the estrogenic action of the 2- phenylbenzothiophene system.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Our Top Choice Compound: 5-Bromobenzothiophene

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4923-87-9, Research speed reading in 2021. The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. In a article, 4923-87-9, molcular formula is C8H5BrS, introducing its new discovery.

The purpose of the present invention is to provide a method for easily producing a fluorine-containing (cyclo)alkenyl zinc halide compound at low cost. The present invention provides a method for producing a fluorine-containing (cyclo)alkenyl zinc halide compound represented by formula (1) (wherein A1 represents a perfluoroalkyl group having 1-12 carbon atoms, or a fluorine atom; A2 represents a fluorine atom or a hydrogen atom; A3 represents a fluorine atom or a hydrogen atom, or alternatively A3 and A1 or A2 may combine together to form a perfluoroalkylene chain having 1-12 carbon atoms; and X’ represents a halogen atom), which comprises a step wherein a fluorine-containing olefin represented by formula (2) (wherein X” represents a fluorine atom or a chlorine atom; and the other symbols are as defined above) is reacted with a zinc halide represented by formula ZnX’2 (wherein the symbol is as defined above) in the presence of one or more metals that are selected from among magnesium and magnesium alloys.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

A new application about 35212-85-2

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Two new series of inhibitors of tubulin polymerization based on the 2-(alkoxycarbonyl)-3-(3?,4?,5?-trimethoxyanilino)benzo[b] thiophene and thieno[2,3-b]pyridine molecular skeletons were synthesized and evaluated for antiproliferative activity on a panel of cancer cell lines, inhibition of tubulin polymerization, cell cycle effects, and in vivo potency. Antiproliferative activity was strongly dependent on the position of the methyl group on the benzene portion of the benzo[b]thiophene nucleus, with the greatest activity observed when the methyl was located at the C-6 position. Also, in the smaller thieno[2,3-b]pyridine series, the introduction of the methyl group at the C-6 position resulted in improvement of antiproliferative activity to the nanomolar level. The most active compounds (4i and 4n) did not induce cell death in normal human lymphocytes, suggesting that the compounds may be selective against cancer cells. Compound 4i significantly inhibited in vivo the growth of a syngeneic hepatocellular carcinoma in Balb/c mice.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Top Picks: new discover of 4923-87-9

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The development of the oxidative cross-coupling of unreactive C(sp3)-H bonds with (hetero)arene C(sp2)-H bonds is considerably appealing, yet conceptually and practically challenging. Here, we disclose the rhodium-catalyzed oxidative heteroarylation of unactivated C(sp3)-H bonds with heteroarene C(sp2)-H bonds. This method provides a step-economic route to beta-heteroarylated 2-ethylpyridine derivatives, which exhibits relatively broad substrate scope, high tolerance level of sensitive functional groups, and high selectivity. The protocol can also be extended to the coupling reaction between 8-methylquinoline derivatives and heteroarenes.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

The Best Chemistry compound: C10H9NO2S

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Phosphodiesterase (PDE) 7 is a high affinity cAMP-specific PDE whose functional role in T-cells has been the subject of some controversy. Recent findings on tissue distribution, however, support the hypothesis that PDE7 could be a good target for the treatment of airway diseases, T-cell related diseases or central nervous system (CNS) disorders. Therefore, the identification of selective inhibitors targeted against PDE7 enzyme has become an attractive area of research. We report here the first use of the descriptors generated by the CODES program for ligand-based virtual screening. This program codifies molecules from a topological point of view and the generated descriptors are related to the chemical nature of the atoms, the atomic bonds and the connectivity with the rest of the molecule. They are also able to distinguish among stereoisomers. By using this approach, 173 compounds were codified, and their similarity with the reference compound was analysed. Based on the analysis, new potential PDE7 inhibitors have been identified, synthesized and biologically evaluated confirming that CODES descriptors are valid for ligand-based virtual screening and provided new lead compounds for further optimization as potent and selective PDE7 inhibitors.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

The important role of C16H14O2S

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The synthesis of benzothiophenes containing a piperazine side chain and their binding affinities for estrogen receptors are described. These compounds bearing piperazine side chains were identified to be high-affinity ligands with high selectivity for ER alpha subtype. They were also potent agonists in bone tissue.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

A new application about C8H5BrS

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A range of bench-stable carbazole-containing hypervalent iodine(III) reagents were synthesized by I ? N bond formation in good yields. This kind of benziodoxolone reagents was used for a C[sbnd]N coupling reaction to introduce a carbazole group to aromatic heterocycle compounds.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

What Kind of Chemistry Facts Are We Going to Learn About 1196-19-6

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[1]Benzothienoindolizidinones 5ac,ae,bc and [1]Benzothienoquinolizidinone 5ad were synthesized from 2(3)-bromethyl[1]benzothiophene and methyl prolinate, methyl oxoprolinate and ethyl pipecolinate. The Schmidt rearrangement of ketones 5 led exclusively to the [1,3]diazepines derivatives 6.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem