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

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Process for preparing 3-(4-aminoethoxy-benzoyl) benzo B!-thiophenes

The invention provides a process for preparing 6-alkoxy-3-(4-alkoxyphenyl)benzo B!thiophenes in good yield on a manufacturing scale without generating a thick, potentially yield-reducing, paste. The invention also provides methods for converting a-(-alkoxyphenylthio)-4-alkoxyacetophenones into 6-hydroxy-2-(4-hydroxyphenyl)-3- 4-(2-aminoethoxy)benzoyl!benzo B!thiophenes via acylation of a dialkoxy benzo B!thiophene. Each of these preparations relies on an intramolecular cyclization of a dialkoxy acetophenone derivative to yield a benzo B!thiophene without generating a thick paste that lowers overall yields on a manufacturing scale.

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Discovery of 5-Bromobenzothiophene

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Palladium-Catalyzed alpha-Arylation of Carboxylic Acids and Secondary Amides via a Traceless Protecting Strategy

A novel traceless protecting strategy is presented for the long-standing challenge of conducting the palladium-catalyzed alpha-arylation of carboxylic aids and secondary amides with aryl halides. Both of the presented coupling processes occur with a variety of carboxylic acids and amides and with a variety of aryl bromides containing a broad range of functional groups, including base-sensitive functionality like acyl, alkoxycarbonyl, nitro, cyano, and even hydroxyl groups. Five commercial drugs were prepared through this method in one step in 81-96% yield. Gram-scale synthesis of medication Naproxen and Flurbiprofen with low palladium loading further highlights the practical value of this method.

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Final Thoughts on Chemistry for 5-Bromobenzothiophene

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USE OF BENZO-HETEROARYL SULFAMIDE DERIVATIVES FOR THE TREATMENT OF PAIN

The present invention is a method for the treatment of pain comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-heteroaryl sulfamide derivatives of formula (I) as herein defined. The present invention is further directed to methods for the treatment of pain comprising co-therapy with analgesic agent(s) and a compound of formula (I) as described herein.

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The Absolute Best Science Experiment for 4923-87-9

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Enzymatic enantioselective decarboxylative protonation of heteroaryl malonates

The enzyme aryl/alkenyl malonate decarboxylase (AMDase) catalyses the enantioselective decarboxylative protonation (EDP) of a range of disubstituted malonic acids to give homochiral carboxylic acids that are valuable synthetic intermediates. AMDase exhibits a number of advantages over the non-enzymatic EDP methods developed to date including higher enantioselectivity and more environmentally benign reaction conditions. In this report, AMDase and engineered variants have been used to produce a range of enantioenriched heteroaromatic alpha-hydroxycarboxylic acids, including pharmaceutical precursors, from readily accessible alpha-hydroxymalonates. The enzymatic method described here represents an improvement upon existing synthetic chemistry methods that have been used to produce similar compounds. The relationship between the structural features of these new substrates and the kinetics associated with their enzymatic decarboxylation is explored, which offers further insight into the mechanism of AMDase. Versatile decarboxylase: Aryl malonate decarboxylase (AMDase) and engineered variants have been shown to catalyse the enatioselective decarboxylative protonation of a range of alpha-heteroaryl alpha-hydroxy malonates with excellent yields and enantioselectivity (see scheme).

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Top Picks: new discover of 2-Bromobenzo[b]thiophene

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Palladium-catalyzed difluoromethylation of heteroaryl chlorides, bromides and iodides

A palladium-catalyzed difluoromethylation of a series of heteroaryl chlorides, bromides and iodides under mild conditions is described. A wide range of heteroaryl halides such as pyridyl, pyrimidyl, pyrazyl, funanyl, thienyl, pyazolyl, imidazolyl, thiazolyl, and oxazolyl halides were efficiently difluoromethylated, thus providing medicinal chemists an alternative choice for the preparation of drug candidates with the difluoromethylated heteroarene unit.

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Extended knowledge of 2,3-Dibromobenzo[b]thiophene

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Synthesis of novel 2-aminoimidazo[4,5-b]pyridines, including the thieno analogue of the cooked-food mutagen IFP

Eight new compounds, including three new ring systems obtained via the Friedlunder condensation of ortto-aminothiophenecarbaldehydes 11, 21 and 24 with creatinine (8), are reported. The condensation afforded 1, which is the thieno analogue of the cooked-food mutagen IFP (2-amino-1,6-dimethylfuro[2,3-e] imidazo[4,5-b]pyridine), and the benzothieno[2,3-e]- and benzothieno[3,2-e] imidazo[4,5-b]pyridines 2 and 3. Attempts to condense 11 with isocreatinine (12) were unsuccesful. Desulfurization of 3 gave the known cooked-food carcinogen PhIP, The 2-nitro (4) and 2-hydroxy (5) derivatives of 3 are reported. The related 2-amino-1-methyl-imidazo[4,5-b]benzothiophene (25) was synthesized by a different route. Fully assigned 1H and 13C nmr data of all new compounds are reported.

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Archives for Chemistry Experiments of 4923-87-9

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Organic light emitting compd. and organic electroluminescence element using the same (by machine translation)

The present invention relates to a novel indole-based compound having excellent hole injection and transport capabilities, light-emission, and other properties, and to an organic electroluminescent device the luminous efficiency, driving voltage, service life, and other characteristics of which are improved due to containing the compound in one or more organic material layers.

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Archives for Chemistry Experiments of 10243-15-9

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Electric Literature of 10243-15-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.10243-15-9, Name is 3-Bromo-2-methylbenzo[b]thiophene, molecular formula is C9H7BrS. In a Article£¬once mentioned of 10243-15-9

Reversibly photoswitchable nucleosides: Synthesis and photochromic properties of diarylethene-functionalized 7-deazaadenosine derivatives

Photochromic nucleosides were designed that combine the structural features and molecular recognition properties of nucleic acids with the light-sensitivity of diarylethenes. Target compounds 1a-c consist of a 7-deazaadenosine unit that is linked to a thiophene as the second aryl functionality via a 1,2-cyclopentenyl linker. These nucleoside analogues undergo a reversible electrocyclic rearrangement, generating strongly colored closed-ring isomers upon irradiation with UV-light, while exposure to light in the visible range triggers the cycloreversion to the colorless opened-ring form. UV-vis spectroscopy, HPLC, and 1H NMR measurements revealed recognition of complementary thymidine and up to 97% conversion to the thermally stable closed-ring isomers after illumination with UV-light. The required wavelength for ring closure was found to vary depending on the substituents attached to the thiophene moiety. In a first design step, we used this important feature of diarylethenes to shift the switching wavelength from initially 300 nm (1a) to 405 nm (1cH+). In a second step, we generated a pair of orthogonal switches, differing enough in their respective switching wavelengths to be controlled independently in the same sample. Finally, a molecular switch was developed that showed both photochromism and acidichromism, thereby illustrating the possibility to gate the spectral properties to multiple stimuli. These new photochromic nucleosides represent useful building blocks for the generation of light-sensitive nucleic acids either by inducing conformational changes upon isomerization or by exploring the different spectral properties of the closed and opened isomers, for example, for use as reversible fluorescence quenchers.

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Selective Heck reaction of electron-rich aryl bromides with cyclic alkenones

A simple and efficient protocol for the Heck reaction of cyclic alkenones with electron-rich aryl bromides has been developed. A ligand combination of X-Phos and tri-tert-butylphosphonium hydrogen tetrafluoroborate in the presence of Pd(PPh3)2Cl2 and Na2CO3 in DMSO was found to be efficient and selective for electron-rich aryl bromides with high substrate scope for cyclic alkenones.

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Final Thoughts on Chemistry for 2,3-Dibromobenzo[b]thiophene

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Benzothiophene compounds as antithrombotic agents and intermediates

This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of the compounds of formula I as thrombin inhibitors. wherein E is CReor N in which Reis hydrogen, methyl, methoxy or halo; R1is hydrogen or methyl; R2is R2aor R2bin which R2ais -X2-(CH2)n-Rfin which X2is a direct bond, methylene or O; n is 1, 2 or 3; and Rfis 5-tetrazolyl, carboxy, [(1-4C)alkoxy]carbonyl or hydroxymethyl; R2bis -X2-(CH2)m-NRaRbin which X2is a direct bond, methylene or O; m is 1, 2 or 3; provided that when m is 1, then X2is a direct bond; and Raand Rbare independently hydrogen or (1-3C)alkyl or the group NRaRbis pyrrolidino, piperidino or morpholino; R3is -X3-(CH2)s-NRsRtin which X3is a direct bond, methylene or O; s is 1 or 2; provided that when s is 1, then X3is a direct bond; and Rsand Rtare independently hydrogen or (1-3C)alkyl or the group NRsRtis pyrrolidino, piperidino or morpholino; and R6is hydrogen, hydroxy or methoxy.

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