Top Picks: new discover of 1034305-17-3

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Discovery of Ipragliflozin (ASP1941): A novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus

A series of C-glucosides with various heteroaromatics has been synthesized and its inhibitory activity toward SGLTs was evaluated. Upon screening several compounds, the benzothiophene derivative (14a) was found to have potent inhibitory activity against SGLT2 and good selectivity versus SGLT1. Through further optimization of 14a, a novel benzothiophene derivative (14h; ipragliflozin, ASP1941) was discovered as a highly potent and selective SGLT2 inhibitor that reduced blood glucose levels in a dose-dependent manner in diabetic models KK-Ay mice and STZ rats.

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Top Picks: new discover of Methyl 4-bromobenzo[b]thiophene-2-carboxylate

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SPIROINDOLINONES AS DDR1 INHIBITORS

The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts thereof, as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.

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Benzothiophene – Wikipedia,
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Imidazolyl-substituted benzothiophenes

The present invention provides novel imidazolyl-benzothiophenes and derivatives thereof which are useful as thromboxane A2 (TXA2) synthetase inhibitors and as such represent potent pharmacological agents.

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Direct route to 1,3-diketones by palladium-catalyzed carbonylative coupling of aryl halides with acetylacetone

Man up your magnesium! By employing a MgCl2/Et3N system, aryl diketones can be generated from the Pd-catalyzed carbonylative alpha-arylation of acetylacetone with aryl bromides (see scheme). The method is ideal for the introduction of carbon isotopes into more complex structures, since only stoichiometric amounts of carbon monoxide are employed. Copyright

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Some scientific research about 2-Bromobenzo[b]thiophene

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Copper/Palladium-Catalyzed Cyclization/Cross-Coupling Cascade Reaction of 2-gem-Dibromovinyl Aryl Selenides: Synthesis of 2-Substituted Benzo[b]selenophenes

Copper/palladium-catalyzed multicomponent cyclization reactions, which combine 2-gem-dibromovinyl aryl selenides with a nucleophilic source, were applied to the synthesis of 2-substituted benzo[b]selenophenes. A systematic study of the cyclization system revealed that the mutual action between copper and palladium salts is essential for the formation of products in good yields, avoiding the formation of hydrogenated benzo[b]selenophenes. The versatility of 2-bromobenzo[b]selenophenes was also studied by palladium-catalyzed reactions with boronic acids, Grignard reagents and methyl acrylate affording the cross-coupled products in good yields. In addition, the reaction of 2-bromobenzo[b]selenophene towards halogen-lithium exchange reactions followed by the addition of aldehyde afforded the corresponding secondary alcohol. (Figure presented.).

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The important role of 63675-74-1

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Process for preparing benzothiophenes

The present invention relates to intermediates and processes for preparing benzothiophenes of the following formula: wherein Y is chloro, bromo, iodo or -SO2R9; and, R9is C1-C4alkyl, trifluoromethyl, trichloromethyl, phenyl, p-tolyl, p-anisyl, or mono- or di(halo or nitro)phenyl.

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A new application about 4923-87-9

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Ni-Mediated Generation of “cN” Unit from Formamide and Its Catalysis in the Cyanation Reactions

The in situ generation of a “cyano” unit from readily available organic precursors is of high interest in synthetic chemistry. Herein, we report the first example of Ni-mediated dehydration of formamide to form “CN” and its subsequent catalytic applications in the hydrocyanation of alkynes and cyanation of aryl halides. Formamide can serve as a convenient source for the nitrile unit, in that it releases water as the only byproduct.

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The Absolute Best Science Experiment for 3-Bromo-2-methylbenzo[b]thiophene

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Synthetic Route 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 Patent£¬once mentioned of 10243-15-9

With the Hg2 + And Cys continuous selective asymmetric perfluoro cyclopentene compound and its preparation method and application (by machine translation)

The invention discloses a [1 – [2 – methyl – 3 – benzothienyl], 2 – (2 – methyl – 5 – (4 – phenyl) – (2 – formyl quinoline – 8 – benzothiazolyl) – 3 – thienyl)] full-PVC pentene and its preparation method and application. Preparation method: to benzo thiophene as raw materials, through the iodomethane substituted, brominated, with the perfluoro pentene reaction to generate single substituted perfluoro pentene; to 2 – methyl thiophene as raw materials, bromination, through the n-BuLi and tributyl borate reaction, Stuzki coupling reaction through the end of the with the thiophene ring containing aldehyde group benzene connected, then with ethylene glycol protection after single substituted perfluoro pentene reaction, by reducing dioxiding hydroxy, any change of containing methyl radical bromine, with 8 – hydroxy quinoline – 2 – aldehyde reaction, finally with 2 – amino thiophenol reaction, to obtain the target compound. Prepared by the invention compounds can be used for continuous detection of a specific ion and amino acid, its selectivity is very good. (by machine translation)

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Extracurricular laboratory:new discovery of Methyl 4-bromobenzo[b]thiophene-2-carboxylate

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SUBSTITUTED INDAZOLE OR INDOLE DERIVATIVES AS IN VITRO MAO-B INHIBITORS

Substituted indazole or imidazole derivatives of formula I as in vitro selective and reversible MAO-B inhibitors and for use in the prevention and treatment of meurodegenerative disorders such as Parkinson’s disease, Alzheimer’s disase and dementia

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

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Efficient Self-Contained Photoacid Generator System Based on Photochromic Terarylenes

A series of highly sensitive neutral photoacid generators (PAGs) based on photochromic terarylenes was prepared. Like the example presented herein, these compounds show a subsequent thermal elimination of a Br¡ãnsted acid after a light-triggered 6pi-electrocyclization, concomitant with the hexatriene aromatization. A novel type of molecular systems was developed, in which one thiazolyl moiety was replaced by a thienyl group. Depending on the solvents and on the nature of the acid source, the quantum yield (QY) for acid generation could reach up to 0.6. Comparative studies on the acid source clearly showed that aromatic leaving groups tend to extinguish the molecular system photoefficiency. A second type was also prepared, in which the nature of the hetero-aromatic rings were identical to our previous example, but their sequence was modified. Therefore, a second level of improvement was achieved in nonpolar solvents, pushing the QY value up to 0.7. Finally, we demonstrated the mesylic acid-releasing PAG as a photocatalyst in a chemically amplified positive resist system.

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Benzothiophene – Wikipedia,
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