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O -Difluorodeuteromethylation of phenols using difluorocarbene precursors and deuterium oxide

The first O-difluorodeuteromethylation of phenols using commercial diethyl bromodifluoromethylphosphonate and deuterium oxide to prepare various difluorodeuteromethyl aryl ethers is reported. This facile method affords a convenient way to introduce OCF2D groups into organic molecules.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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PYRIMIDINE DERIVATIVES AS PGE2 RECEPTOR MODULATORS

The present invention relates to pyrimidine derivatives of formula (I) wherein (R1)n, R3, R4a, R4b, R5a, R5b and Ar1 are as described in the description and their use in the treatment of cancer by modulating an immune response comprising a reactivation of the immune system in the tumor. The invention further relates to novel benzofurane and benzothiophene derivatives of formula (II) and their use as pharmaceuticals, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

More research is needed about Benzo[b]thiophen-5-ol

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 19301-35-0, and how the biochemistry of the body works.Application of 19301-35-0

Application of 19301-35-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.19301-35-0, Name is Benzo[b]thiophen-5-ol, molecular formula is C8H6OS. In a Article£¬once mentioned of 19301-35-0

Specific estrogen sulfotransferase (SULT1E1) substrates and molecular imaging probe candidates

This work focuses on the development of specific substrates for estrogen sulfotransferase (SULT1E1) to produce molecular imaging probes for this enzyme. SULT1E1 is a key enzyme in estrogen homeostasis, playing a central role in the prevention and development of human disease. In vitro sulfation assays showed alkyl and aryl substitutions to a fused heterocyclic system modeled after beta-naphthol (betaN), based on compounds that interact with the estrogen receptor, rendered several molecules with enhanced specificity for SULT1E1 over SULT1A1*1, SULT1A1*2, SULT1A3, and SULT2A1. Several 6-hydroxy-2-arylbenzothiazoles tested demonstrated excellent affinity – V max/Km ratios – and specificity for SULT1E1. Km values ranged from 0.12-2.36 muM. A strong correlation was observed between polarity of the 4?-sustituent on the 2-aryl moiety (Hammett sigmap) and the log(Vmax/Km) (r = 0.964). Substrate sensitivity is influenced by the acidity of the 6-phenolic group demonstrated by correlating its 1H NMR chemical shift (deltaOH) with the log(V max/Km) (r = 0.963). Acidity is mediated by the electron withdrawing capacity of the 4?-substituent outlined by the correlation of the C-2 13C NMR chemical shift (deltaC2) with the log(Vmax/Km) (r = 0.987). 2-[4-(Methylamino)phenyl]-6- hydroxybenzothiazole (2b) was radiolabeled with carbon-11 (11C-(2b)) and used in vivo for microPET scanning and tissue metabolite identification. High PET signal was paralleled with the presence of radiolabeled 11C-(2b)-6-O-sulfate and the SULT1E1 protein detected by western blot. Because this and other members of this family presenting specificity for SULT1E1 can be labeled with carbon-11 or fluorine-18, in vivo assays of SULT1E1 functional activity are now feasible in humans.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Pd-catalyzed synthesis of aryl and heteroaryl triflones from reactions of sodium triflinate with aryl (heteroaryl) triflates

A novel method for Pd-catalyzed triflination of aryl and heteroaryl triflates using NaSO2CF3 as the nucleophile is described. The combination of Pd2(dba)3 and RockPhos formed the most effective catalyst. A broad range of functional groups and heteroaromatic compounds were tolerated under the neutral reaction conditions. The order of reactivity ArOTf ? ArCl ? ArBr is consistent with transmetalation being a slow step of the reaction.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 19301-35-0, and how the biochemistry of the body works.HPLC of Formula: C8H6OS

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4-Benzofuranyloxynicotinamide derivatives are novel potent and orally available TGR5 agonists

A series of 4-benzofuranyloxynicotinamide derivatives were identified to be novel, potent, and orally available TGR5 agonists. Among them, compound 9r had the highest potency in vitro (hTGR5 EC50 = 0.28 nM, mTGR5 EC 50 = 0.92 nM). Further in vivo studies disclosed that 9r could effectively lower the blood glucose, but meantime caused an increase in the gallbladder volume of mice. Subsequent research toward eliminating the gallbladder toxicity resulted in compound 19 with low permeability. Although the EC50 of mTGR5 of 19 was larger one order than that of 9r, it still had good glucose-lowing activity. Nevertheless, 19 also caused the adverse effects to the gallbladder. The drug levels detection disclosed that the concentration of 19 was only lower than that of 9r in plasma but was higher in bile and gallbladder tissue. This result indicated that low exposure in plasma could not guarantee low exposure in bile and gallbladder tissue, and thus resulting in the gallbladder toxicity of 19.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Studies in Sulphur Heterocycles: Part III – Syntheses of Tricyclic Compounds with Condensed Thiophene Rings

Some members of the thieno<3,2-e><1>benzothiophene, <1>benzothieno<3,2-b>pyrrole, thieno<2,3-g>-1,2-benzisoxazole and thieno<2,3-g>indazole ring systems have been synthesized from 6,7-dihydrobenzothiophen-4(5H)-one derivatives.The unsaturated ethers of 4- and 5-hydroxybenzothiophenes undergo Claisen rearrangement followed by ring closure to give thieno<2,3-h><1>benzopyran and thieno<3,2-e><1>benzopyran ring systems.Syntheses of new thienobenzofurans from 4-hydroxybenzothiophene-5-carbaldehyde, its 2-methyl derivative and 5-hydroxybenzothiophene-4-carbaldehyde are also described.

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

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 19301-35-0, and how the biochemistry of the body works.Application of 19301-35-0

Application of 19301-35-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.19301-35-0, Name is Benzo[b]thiophen-5-ol, molecular formula is C8H6OS. In a Article£¬once mentioned of 19301-35-0

Synthesis and SAR studies of bicyclic amine series GPR119 agonists

We disclosed a novel series of G-protein coupled receptor 119 (GPR119) agonists based on a bicyclic amine scaffold. Through the optimization of hit compound 1, we discovered that the basic nitrogen atom of bicyclic amine played an important role in GPR119 agonist activity expression and that an indanone in various bicyclic rings was suitable in this series of compounds. The indanone derivative 2 showed the effect of plasma glucose control in oGTT and scGTT in the rodent model.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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BENZODIOXEPINE AND BENZODIOXINE COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN FOR THE TREATMENT OF DIABETES

The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Synthesis and biological evaluation of novel small non-peptidic HIV-1 PIs: The benzothiophene ring as an effective moiety

Synthesis and biological evaluation of a new series of potential HIV-1 protease inhibitors incorporating different heterocycles are described. The variation of heteroatom in such molecules has displayed totally different biological activities and a benzothiophene containing inhibitor has shown high potency against wild type HIV-1 protease with IC50 = 60 nM, thanks to the lower desolvation penalty to be payed by such hydrophobic moiety.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 19301-35-0, and how the biochemistry of the body works.Reference of 19301-35-0

Reference of 19301-35-0, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 19301-35-0, Name is Benzo[b]thiophen-5-ol,introducing its new discovery.

O -Difluorodeuteromethylation of phenols using difluorocarbene precursors and deuterium oxide

The first O-difluorodeuteromethylation of phenols using commercial diethyl bromodifluoromethylphosphonate and deuterium oxide to prepare various difluorodeuteromethyl aryl ethers is reported. This facile method affords a convenient way to introduce OCF2D groups into organic molecules.

We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 19301-35-0, and how the biochemistry of the body works.Reference of 19301-35-0

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