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Synthesis of 7-oxo-dihydrospiro[indazole-5,4?-piperidine] acetyl-CoA carboxylase inhibitors

Synthesis of oxo-dihydrospiroindazole-based acetyl-CoA carboxylase (ACC) inhibitors is reported. The dihydrospiroindazoles were assembled in a regioselective manner in six steps from substituted hydrazines and protected 4-formylpiperidine. Enhanced regioselectivity in the condensation between a keto enamine and substituted hydrazines was observed when using toluene as the solvent, leading to selective formation of 1-substituted spiroindazoles. The 2-substituted spiroindazoles were formed selectively from alkyl hydrazones by ring closure with Vilsmeier reagent. The key step in the elaboration to the final products is the conversion of an intermediate olefin to the desired ketone through elimination of HBr from an O-methyl bromohydrin. This methodology enabled the synthesis of each desired regioisomer on 50-75 g scale with minimal purification. Acylation of the resultant spirocyclic amines provided potent ACC inhibitors.

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

 

Extended knowledge of 5-Bromobenzothiophene

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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

 

Awesome and Easy Science Experiments about 5-Bromobenzothiophene

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Oxalic Diamides and tert-Butoxide: Two Types of Ligands Enabling Practical Access to Alkyl Aryl Ethers via Cu-Catalyzed Coupling Reaction

A robust and practical protocol for preparing alkyl aryl ethers has been developed, which relies on using two types of ligands to promote Cu-catalyzed alkoxylation of (hetero)aryl halides. The reaction scope is very general for a variety of coupling partners, particularly for challenging secondary alcohols and (hetero)aryl chlorides. In case of coupling with aryl chlorides and bromides, two oxalic diamides serve as the powerful ligands. The tert-butoxide is first demonstrated as a ligand for Cu-catalyzed coupling reaction, leading to alkoxylation of aryl iodides complete at room temperature. Additionally, a number of carbohydrate derivatives are applicable for this coupling reaction, affording the corresponding carbohydrate-aryl ethers in 29-98% yields.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Extended knowledge of 6287-82-7

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Concise synthesis of highly substituted benzo[a]quinolizines by a multicomponent reaction/allylation/heck reaction sequence

The combination of the recently developed multicomponent construction of highly substituted 3,4-dihydropyridones with subsequent allylation and intramolecular Heck-type cyclization allows the straightforward construction of benzo[a]quinolizines, a class of polycyclic compounds that- despite their interesting pharmacological and photochemical properties- have little precedent in the literature. After optimization of the individual steps, we used this reliable three-step sequence to generate a small library of diversely substituted benzo[a]quinolizines and various heterocyclic analogs. Copyright

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Extracurricular laboratory:new discovery of Methyl 7-nitrobenzo[b]thiophene-2-carboxylate

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Electric Literature of 34084-89-4, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.34084-89-4, Name is Methyl 7-nitrobenzo[b]thiophene-2-carboxylate, molecular formula is C10H7NO4S. In a Patent£¬once mentioned of 34084-89-4

Preparation method of 7- piperazine benzothiophene or salt thereof (by machine translation)

7 – Shows the preparation method of,piperazine benzothiophene or a salt thereof, wherein :(1) compound 3 and compound 4 are subjected to hydrolysis decarboxylation, to obtain compound 5;(2) compound 5, and compound, is subjected to a nitro-reduction reaction 6;(3) to obtain compound 6 compound, and compound 7;(4) through a multi-step reaction. 7. The preparation method disclosed by the invention can be used as starting material 8 – 1 to prepare,piperazinylbenzothiophene or salt, thereof through multi-step reaction to obtain the compound . The preparation method disclosed by the invention is simple and, convenient 7 – operation and, DEG C. (by machine translation)

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

 

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1. 3 – Disubstituted ketenes compound and use thereof (by machine translation)

The invention relates to a kind of formula (I) of the structure shown in Figure 1, 3 – disubstituted compound ketenes and its application. The compounds mainly activated PPAR alpha, to the PPPA delta and PPPA gamma have agonistic activity. Can be used for the treatment of PPAR regulating abnormal various diseases associated, such as non-alcoholic fatty liver disease particularly in the treatment of non-alcoholic hepatitis, also used for the treatment of diabetes, obesity, fibrotic diseases, cardiovascular disease (including heart failure and atherosclerosis and the like), kidney disease (including chronic renal disease and renal failure and the like), cerebral degenerative diseases (including Alzheimer’s disease and the like) such as the potential of the, has great application value. (by machine translation)

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Properties and Exciting Facts About 3-(Bromomethyl)benzo[b]thiophene

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Related Products of 1196-19-6, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 1196-19-6, Name is 3-(Bromomethyl)benzo[b]thiophene, molecular formula is C9H7BrS. In a Patent£¬once mentioned of 1196-19-6

PROCESS FOR THE PREPARATION OF SULFAMIDE DERIVATIVES

The present invention is directed to novel processes for the preparation of sulfamide derivatves, useful in the treatment of epilepsy and related disorders.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Extracurricular laboratory:new discovery of 360576-01-8

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Recommanded Product: 360576-01-8, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 360576-01-8, name is Methyl 6-bromobenzo[b]thiophene-2-carboxylate. In an article£¬Which mentioned a new discovery about 360576-01-8

INHIBITORS OF LOW MOLECULAR WEIGHT PROTEIN TYROSINE PHOSPHATASE (LMPTP) AND USES THEREOF

Protein tyrosine phosphatases (PTPs) are key regulators of metabolism and insulin signaling. As a negative regulator of insulin signaling, the low molecular weight protein tyrosine phosphatase (LMPTP) is a target for insulin resistance and related conditions. Described herein are compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and compositions, and methods of using these compounds and compositions.

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

 

Extended knowledge of 4923-87-9

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Enantioselective Radical Ring-Opening Cyanation of Oxime Esters by Dual Photoredox and Copper Catalysis

Catalytic enantioselective chemical reactions involving highly reactive radical species remain largely unexplored. We report herein for the first time a novel enantioselective radical ring-opening cyanation of redox-active oxime esters by dual photoreodox and copper catalysis. This mild protocol shows good functional group tolerance and broad substrate scope, producing a wide range of optically active alkyl dinitriles with high yields and excellent enantioselectivities, which are difficult to access traditionally.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

A new application about 6287-82-7

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Reference of 6287-82-7, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 6287-82-7, Name is 2,3-Dibromobenzo[b]thiophene, molecular formula is C8H4Br2S. In a Article£¬once mentioned of 6287-82-7

Photon-Quantitative 6pi-Electrocyclization of a Diarylbenzo[b]thiophene in Polar Medium

The high reactivity of 6pi-electrocyclization in polar solvents has remained one of the important challenges for diarylethenes because of the emergence of a twisted intramolecular charge transfer (TICT) state at the excited state in such polar media, which usually quenches the photocyclization reaction. Herein we report on the preparation and highly efficient photocyclization of 2,3-diarylbenzo[b]thiophenes with nonsymmetric side-aryl units in a polar solvent. While the dithiazolylbenzo[b]thiophene showed a suppressed quantum yield of 6pi-electrocyclization of 54% in methanol, the replacement of a thiazole unit with a thiophene ring led to a photon-quantitative 6pi-cyclization reaction. The nonsymmetrical modification into the side-aryl units was considered to enhance the CH/pi interactions between side-aryl units to support a photoreactive conformation in methanol. The stabilization of the photochromic reactive conformation is expected to suppress the formation of the TICT state at the excited state, leading to highly efficient photoreactivity.

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