What I Wish Everyone Knew About C10H9NO2S

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Microwave irradiation of 2-halobenzonitriles and methyl thioglycolate in the presence of triethylamine in DMSO at 130C provides rapid access to 3-aminobenzo[b]thiophenes in 58-96% yield. This transformation has been applied in the synthesis of the thieno[2,3-b]pyridine core motif of LIMK1 inhibitors, the benzo[4,5]thieno[3,2-e][1,4]diazepin-5(2H)-one scaffold of MK2 inhibitors and a benzo[4,5]thieno[3,2-d]pyrimidin-4-one inhibitor of the PIM kinases.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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The use of substances capable of inhibiting one or more enzymes of the histone deacetylase family (histone deacetylase inhibitors) for the therapeutic treatment of Philadelphia-negative myeloproliferative syndromes (polycythemia vera, essential thrombocythemia or idiopathic myelofibrosis) is described. The dosage of the above-mentioned substances is significantly lower than that normally used for the care of other tumor syndromes and may be from 10 to 150 mg/day/patient.

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A newly engineered palladacycle that contains substituents on the biphenyl rings along with the ligand HandaPhos is especially well-matched to an aqueous micellar medium, enabling valued Suzuki-Miyaura couplings to be run not only in water under mild conditions, but at 300 ppm of Pd catalyst. This general methodology has been applied to several targets in the pharmaceutical area. Multiple recyclings of the aqueous reaction mixture involving both the same as well as different coupling partners is demonstrated. Low temperature microscopy (cryo-TEM) indicates the nature and size of the particles acting as nanoreactors. Importantly, given the low loadings of Pd invested per reaction, ICP-MS analyses of residual palladium in the products shows levels to be expected that are well within FDA allowable limits.

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What Kind of Chemistry Facts Are We Going to Learn About 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

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The crystal and molecular structures of two methoxybenzo [b] thiophenes have been determined by three-dimensional, single-crystal X-ray diffractometry. Both 3-(3?,4?,5?-trimethoxybenzoyl)-2-(4?-methoxyphenyl)-6- methoxybenzo[b]thiophene and 3-(3?,4?,5?-triethoxybenzoyl)-2-(4?-methoxyphenyl)-6- methoxybenzo[b]thiophene (hereafter referred to as I and II, respectively) crystallize in the triclinic centrosymmetric space group P1 (No. 2, C1) with two formula units per cell with a = 6.842(1) A, b = 12.602(2) A, c = 13.815(2) A, alpha = 94.80(1), beta = 98.27(2), and gamma = 100.59(2) and a = 10.600(1), b = 11.415(2), c = 12.137(2) A, alpha = 94.57(1), beta = 101.18(1), and gamma = 110.45(1), respectively. The phase problems were solved by direct methods and the respective final full-matrix least-squares refinements converged to R = 0.039 and 0.068. The structures differ in the orientation of the trimethoxy and triethoxy groups of the benzoyl ligands. The molecules in the crystal lattice are held together by van der Waals forces. Selected bond distances, angles, and torsion angles are tabularized as well as reference to the synthesis of the title compounds and peripheral studies.

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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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A novel potent NMDA-NR2B selective antagonist (5b) without the reactive metabolites formation issue was identified. Through this study, a close correlation between reactive metabolites formation and calculated HOMO energies of parent compounds was found.

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Why Are Children Getting Addicted To C15H10BrFOS

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The invention discloses a 2 – (5 – bromo – 2 – fluorobenzyl) benzo thiophene synthetic method, in order to 2 – fluoro – 5 – bromobenzene as a raw material, under the action of alkali through condensation and reduction shall be the target compound, comprising a condensation reaction and the reduction reaction, the present invention only two-step reaction to obtain the target compound, reduces the material varieties, improving the operating efficiency. The present invention not using a boron trifluoride ether and other chemicals, and does not use the like sodium borohydride as the reducing agent is not suitable for industrial scale, without the need for ultra-low temperature thereby reducing the production cost, in short synthetic method of this invention has mild reaction condition, simple process operation, environmental protection, low cost, and high yield. (by machine translation)

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The present invention provides a compound, that is a 1-({halo-2-[(2-hydrocarbyl or substituted hydrocarbyl)oxy]phenyl}methyl)-(fused bicyclic nitrogen heteroaryl) carboxylic acid or an ester or sulfonamide thereof. The compound may be represented by the following formula I, Wherein R1, R2, R3, R4 A, X, W, Z and Y are as defined in the specification. The compounds may be administered to treat DP, FP, EP1, TP and/or EP4 receptor-mediated diseases or conditions.

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Extended knowledge of Methyl 5-(trifluoromethyl)benzo[b]thiophene-2-carboxylate

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This invention provides a compound the formula (I), wherein R1 represents an aryl group having from 6 to 10 ring carbon atoms etc.; R2 represents a hydrogen atom etc., n epresents 0, 1 or 2; said heteroaryl group is unsubstituted or substituted and said ary is substituted by at least one substituer,t selected from the group consisting of substituents a; said substituents a are selected from the group 10 consisting of halogen ate ms, alkyl groups having from 1 to 6 carbon atoms etc.; or a pharmaceutically ac eptable ester of such compound, or a pharmaceutically ac eptable salt thereof. These compou ds are useful for the treatment of disease conditions caused 15 by overactivation of N DA NR2B receptor such of pain, stroke, traumatic brain injury, Parkinson’s disease, Alzheimer’s disease, depression, anxiety, migraine, or the like in mammalian, especially humans. This invention also provides a pharmaceutical composi ion comprising the above compound.

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Benzothiophene – Wikipedia,
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Never Underestimate The Influence Of 2-Bromobenzo[b]thiophene

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A convenient procedure for the synthesis of N-(2-cyanoaryl)benzamides has been developed. Using aryl bromides and 2-aminobenzonitriles as the substrates, Mo(CO)6 as the CO source, the desired amides were produced in good yields. Quinazolinones were produced in good yields in a sequential manner as well.

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