Category: benzothiophene

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Product Details of 4923-87-9. Introducing a new discovery about 4923-87-9, Name is 5-Bromobenzothiophene

General and Practical Potassium Methoxide/Disilane-Mediated Dehalogenative Deuteration of (Hetero)Arylhalides

Herein we describe a general, mild and scalable method for deuterium incorporation by potassium methoxide/hexamethyldisilane-mediated dehalogenation of arylhalides. With CD3CN as a deuterium source, a wide array of heteroarenes prevalent in pharmaceuticals and bearing diverse functional groups are labeled with excellent deuterium incorporation (>60 examples). The ipso-selectivity of this method provides precise access to libraries of deuterated indoles and quinolines. The synthetic utility of our method has been demonstrated by the incorporation of deuterium into complex natural and drug-like compounds.

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Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. HPLC of Formula: C8H6OS. Introducing a new discovery about 130-03-0, Name is Benzo[b]thiophen-3(2H)-one

Does aromaticity in a reaction product increase or decrease the intrinsic barrier? Kinetics of the reversible deprotonation of benzofuran-3(2H)-one and benzothiophene-3(2H)-one

A kinetic study of the reversible deprotonation of benzofuran-3(2H)-one (3H-O) and benzothiophene-3(2H)-one (3H-S) by amines and hydroxide ion in water at 25 C is reported. The respective conjugate bases, 3–O and 3–S, represent benzofuran and benzothiophene derivatives, respectively, and thus are aromatic. The main question addressed in this paper is whether this aromaticity has the effect of enhancing or lowering intrinsic barriers to proton transfer. These intrinsic barriers were either determined from Bronsted plots for the reactions with amines or calculated on the basis of the Marcus equation for the reaction with OH-; they were found to be lower for the more highly aromatic benzothiophene derivative, indicating that aromaticity lowers the intrinsic barrier. It is shown that the reduction in the intrinsic barrier is not an artifact of other factors such as inductive, steric, resonance, polarizability, and pi-donor effects, although these factors affect the intrinsic barriers in a major way. Our results imply that aromatic stabilization of the transition state is ahead of proton transfer; this contrasts with simple resonance effects, which typically lag behind proton transfer at the transition state, thereby increasing intrinsic barriers.

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Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Synthetic Route of 104795-85-9, 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, 104795-85-9, Methyl 6-chlorobenzo[b]thiophene-2-carboxylate, introducing its new discovery.

Discovery of fluorescent coumarin-benzo[b]thiophene 1, 1-dioxide conjugates as mitochondria-targeting antitumor STAT3 inhibitors

STAT3 has been extensively studied as a potential antitumor target. Though studies on regulating STAT3 mainly focus on the inhibition of STAT3 phosphorylation at Tyr705 residue, the phosphorylation at Ser727 residue of STAT3 protein is also closely associated with the mitochondrial import of STAT3 protein. N, N-diethyl-7-aminocoumarin is a fluorescent mitochondria-targeting probe. In this study, a series of STAT3 inhibitors were developed by connecting N, N-diethyl-7-aminocoumarin fluorophore with benzo [b]thiophene 1, 1-dioxide moiety. All designed compounds displayed potent anti-proliferative activity against cancer cells. The representative compound 7a was mainly accumulated in mitochondria visualized by its fluorescence. STAT3 phosphorylation was inhibited by compound 7a at both Tyr705 and Ser727 residues. Compound 7a inhibited STAT3 phosphorylation whereas had no influence on the phosphorylation levels of STAT1, JAK2, Src and Erk1/2, indicating good selectivity of compound 7a. Moreover, compound 7a down-regulated the expression of STAT3 target genes Bcl-2 and Cyclin D1, increased ROS production and remarkably reduced the mitochondrial membrane potential to induce mitochondrial apoptotic pathway. Furthermore, compound 7a in vivo suppressed breast cancer 4T1 implanted tumor growth. Taken together, these results highlighted that compound 7a might be a promising mitochondria-targeting STAT3 inhibitor for cancer therapy.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Synthetic Route of 104795-85-9. In my other articles, you can also check out more blogs about 104795-85-9

Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Safety of 5-Bromobenzothiophene. Introducing a new discovery about 4923-87-9, Name is 5-Bromobenzothiophene

Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors

(Chemical Equation Presented) A series of 4-bicyclic heteroaryl 1,2,3,4-tetrahydroisoquinoline inhibitors of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT) was discovered. The synthesis and structure-activity relationship (SAR) of these triple reuptake inhibitors (TRIs) will be discussed. Compound 10i (AMR-2), a very potent inhibitor of SERT, NET, and DAT, showed efficacy in the rat forced-swim and mouse tail suspension models with minimum e ffective doses of 0.3 and 1 mg/kg (po), respectively. At efficacious doses in these assays, 10i exhibited substantial occupancy levels at the three transporters in both rat and mouse brain. The study of the metabolism of 10i revealed the formation of a significant active metabolite, compound 13.

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Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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.

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Safety of Benzo[b]thiophen-4-amine, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 17402-83-4, in my other articles.

Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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. HPLC of Formula: C8H6OS, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 130-03-0, Name is Benzo[b]thiophen-3(2H)-one, molecular formula is C8H6OS

Synthesis of cyclic thioethers through tandem C(sp3)-S and C(sp2)-S bond formations from alpha,beta?-dichloro vinyl ketones

(Chemical Equation Presented) The synthesis of 5- to 8-memebered cyclic thioethers 4 has been achieved through a simple two-step sequence. The present methodology utilizes the facile Friedel-Crafts acylation of terminal alkynes 1 with acid chlorides 2 followed by tandem C(sp3)-S and C(sp 2)-S bond formations with NaSH·xH2O.

One of the oldest and most widely used commercial enzyme inhibitors is aspirin, HPLC of Formula: C8H6OS, which selectively inhibits one of the enzymes involved in the synthesis of molecules that trigger inflammation. you can also check out more blogs about 130-03-0

Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. COA of Formula: C8H5BrS, In an article, mentioned the application of 5394-13-8, Name is 2-Bromobenzo[b]thiophene, molecular formula is C8H5BrS

Palladium-Catalyzed Carbonylative alpha-Arylation of tert -Butyl Cyanoacetate with (Hetero)aryl Bromides

A three-component coupling protocol has been developed for the generation of 3-oxo-3-(hetero)arylpropanenitriles via a carbonylative palladium-catalyzed alpha-arylation of tert-butyl 2-cyanoacetates with (hetero)aryl bromides followed by an acid-mediated decarboxylation step. Through the combination of only a stoichiometric loading of carbon monoxide and mild basic reaction conditions such as MgCl2 and dicyclohexylmethylamine for the deprotonation step, an excellent functional group tolerance was ensured for the methodology. Through the use of 13C-labeled carbon monoxide generated from 13COgen, the corresponding 13C-isotopically labeled beta-ketonitriles were obtained, and these products could subsequently be converted into cyanoalkynes and 3-cyanobenzofurans with site specific 13C-isotope labeling. (Chemical Equation Presented).

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Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Application of 19301-35-0, 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, 19301-35-0, Benzo[b]thiophen-5-ol, introducing its new discovery.

Addition Reactions of Benzothiophen. Part 4. Reactions of Some Acetoxy- and Hydroxy-benzothiophens with Benzene or Toluene

Heating acetoxybenzothiophens with AlCl3-benzene can give the normal Fries-rearranged products (for the 4-OAc and 7-OAc isomers); these sometimes react further to give their 2,3-dihydro- (for 4-OAc and 7-OAc) or 2-phenyl derivatives (for 6-OAc).Alternatively, benzene can add across the 2,3-double bond of the acetoxy-compound, to give the 2- (for 6-OAc) or 3-phenyl-2,3-dihydrobenzothiophens (for 7-Oac).With AlCl3 in dichloromethane, 6-acetoxybenzothiophen undergoes intermolecular transfer of an acetyl group to give a mixture of 6-acetoxy-2- and 3-acetylbenzothiophens and 6-hydroxybenzothiophen.With AlCl3 in benzene at room temperature, 4-acetoxybenzothiophen gives a rearranged product, 4,5-dihydro-2,4-diphenylbenzothiophen-7(6H)-one (3a) (17percent).In the presence of AlCl3 for 0.5 h, 4-, 5-, 6-, and 7-hydroxybenzothiophens undergo addition of benzene or toluene, to give the appropriate 2-aryl-2,3-dihydrohydroxybenzothiophens (1).Yields are high for the 4- and 6-hydroxy-isomers (80-85percent), but lower for the 5- (55percent) and 7-isomers (10percent).In each of these reactions the starting hydroxybenzothiophen is partly converted into its 2,3-dihydro-derivative. 5- and 7-Hydroxybenzothiophen also each give the same 4,5-dihydro-2,4-diarylbenzothiophen-7(6H)-one (3) (25percent) in this reaction.When the reaction period with benzene or toluene is extended to 5 days, the amount of solvent addition product (1) decreases, but all four hydroxy-isomers now give the same rearranged product (3).The mechanism of this unusual rearrangement is discussed in terms of a spiro-intermediate.

Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Application of 19301-35-0. In my other articles, you can also check out more blogs about 19301-35-0

Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem