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N-Arylation of Carbamates through Photosensitized Nickel Catalysis

A highly efficient method of visible light mediated Ni(II)-catalyzed photoredox N-arylation of Cbz-amines/Boc-amines with aryl electrophiles at room temperature is reported. The methodology provides a common access to a wide variety of N-aromatic and N-heteroaromatic carbamate products that find use in the synthesis of several biologically active molecules and provides a distinct advantage over traditional palladium-catalyzed Buchwald reaction.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Copper(I) Oxide/N,N?-Bis[(2-furyl)methyl]oxalamide-Catalyzed Coupling of (Hetero)aryl Halides and Nitrogen Heterocycles at Low Catalytic Loading

An easily prepared oxalic diamide is a powerful ligand for the copper-catalyzed coupling of aryl halides with nitrogen heterocycles. Only 1?2 mol% each of copper(I) oxide and N,N?-bis[(2-furyl)methyl]oxalamide (BFMO) are needed to form N-arylation products under mild conditions. More than 10 different types of nitrogen heterocycles are compatible with these conditions, thereby giving the corresponding N-arylation products. (Figure presented.).

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Asymmetric Allylic C-H Alkylation via Palladium(II)/ cis-ArSOX Catalysis

We report the development of Pd(II)/cis-aryl sulfoxide-oxazoline (cis-ArSOX) catalysts for asymmetric C-H alkylation of terminal olefins with a variety of synthetically versatile nucleophiles. The modular, tunable, and oxidatively stable ArSOX scaffold is key to the unprecedented broad scope and high enantioselectivity (37 examples, avg. > 90% ee). Pd(II)/cis-ArSOX is unique in its ability to effect high reactivity and catalyst-controlled diastereoselectivity on the alkylation of aliphatic olefins. We anticipate that this new chiral ligand class will find use in other transition metal catalyzed processes that operate under oxidative conditions.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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PIPERIDINE DERIVATIVES FOR GPR119 AGONIST

The present invention relates to novel piperidine derivatives, stereoisomers thereof or pharmaceutically acceptable salts thereof; methods for preparing the compound; and pharmaceutical compositions comprising the compound. The novel piperidine derivatives, according to the present invention, having an effect as GPR119 agonist can be used for treatment of metabolic disorders, including diabetes mellitus (especially type II) and related disorders.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Reactive liquid crystal of the original, comprising the liquid crystal composition and liquid crystal display device (by machine translation)

The invention relates to a reactive liquid crystal of the original, comprising the liquid crystal composition and liquid crystal display device. The reasons for the above-mentioned reactive liquid crystal chemical formula 1 expressed: in chemical formula 1 in, X1 And X2 Each independently is hydrogen or halogen, Y is – O -, – S -, – NH – or – SiH2 -, For the 1, 4 – sub-cyclohexyl, or at least one hydrogen halogen-substituted or unsubstituted 1, 4 – phenylene, l is 0 or 1 integer, P1 And P2 For the same or different each other polymerizable functional group, SP1 And SP2 Are each independently a single bond or is selected from 1 to 15 carbon atoms in the alkyl linear chain asia for any one of the bivalent radical, or the divalent radical in which at least one hydrogen halogen or cyano substituted or the at least one – CH2 The oxygen atom is not directly connected to the – manner – C ? C -, – CH=CH -, – O -, – CO – O -, – O – CO – or – O – CO – O – unsubstituted divalent radical. Chemical formula 1 (by machine translation)

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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four links two tie compound and its preparation and use (by machine translation)

The present invention is pharmaceutical chemistry, pharmacology with the preparation field, in particular to four links two tie compound, preparation, pharmacological mechanism of action studies, application, preparation, relates to four links two tie compounds for treatment of anticoagulant, cerebral ischemia, cerebral apoplexy, cerebral edema, cerebral infarction, injury of the neural function. (by machine translation)

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Photochemical Nickel-Catalyzed Reductive Migratory Cross-Coupling of Alkyl Bromides with Aryl Bromides

A novel method to access 1,1-diarylalkanes from readily available, nonactivated alkyl bromides and aryl bromides via visible-light-driven nickel and iridium dual catalysis, wherein diisopropylamine (iPr2NH) is used as the terminal stoichiometric reductant, is reported. Both primary and secondary alkyl bromides can be successfully transformed into the migratory benzylic arylation products with good selectivity. Additionally, this method showcases tolerance toward a wide array of functional groups and the presence of bases.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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CYP17 inhibitors. Annulations of additional rings in methylene imidazole substituted biphenyls: Synthesis, biological evaluation and molecular modelling

Twenty-one novel compounds originating from two classes of annulated biphenyls were synthesized as mimetics of the steroidal A- and C-rings and examined for their potency as inhibitors of human CYP17. Selected compounds were tested for inhibition of the hepatic CYP enzyme 3A4. Potent CYP17 inhibitors were found for each class, compound 9 (17 and 71% at 0.2 and 2 muM, respectively) and 21 (591 nM). Compound 21 showed only weak inhibition of CYP3A4 (32 and 64% at 2 and 10 muM, respectively). Both compounds, however, exhibited moderate to strong inhibition of the glucocorticoid-forming enzyme CYP11B1. The most interesting compounds were docked into our protein model. They bound into one of the modes which we have previously published. New interaction regions were identified.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Migratory Arylboration of Unactivated Alkenes Enabled by Nickel Catalysis

An unprecedented arylboration of unactivated terminal alkenes, featuring 1,n-regioselectivity, has been achieved by nickel catalysis. The nitrogen-based ligand plays an essential role in the success of this three-component reaction. This transformation displays good regioselectivity and excellent functional-group tolerance. In addition, the incorporation of a boron group into the products provides substantial opportunities for further transformations. Also demonstrated is that the products can be readily transformed into pharmaceutically relevant molecules. Unexpectedly, preliminary mechanistic studies indicate that although the metal migration favors the alpha-position of boron, selective and decisive bond formation is favored at the benzylic position.

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Benzothiophene – Wikipedia,
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Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction. In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. 4923-87-9, name is 5-Bromobenzothiophene. In an article£¬Which mentioned a new discovery about 4923-87-9, Product Details of 4923-87-9.

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