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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Benzothiophene – Wikipedia,
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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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Properties and Exciting Facts About 5-Bromobenzothiophene

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RhCl3-Catalyzed Oxidative C-H/C-H Cross-Coupling of (Hetero)aromatic Sulfonamides with (Hetero)arenes

1,1?-Bi(hetero)aryl 2-sulfonamide scaffolds have been widely used as a privileged structure in drug discovery. Herein, we report an efficient rhodium-catalyzed oxidative C-H/C-H cross-coupling between a (hetero)aromatic sulfonamide and a (hetero)arene to afford ortho-sulfonamido bi(hetero)aryls. This methodology features broad substrate scope, good functional group tolerance, and relatively inexpensive catalyst (without the use of RhCp). A wide range of (hetero)arenes such as thiophenes, benzothiophenes, pyrroles, furans, benzofuran, indolizine, and simple arenes can engage in this transformation. This protocol also provides a facile route to bi(hetero)aryl sultams and dibenzo[b,d]thiophene 5,5-dioxides through further intramolecular cyclization, indicating its potential application in materials exploitation.

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Some scientific research about Benzo[b]thiophen-3(2H)-one

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EFFECT OF ANNELATION ISOMERISM ON OPTICAL PROPERTIES OF SOME THIONAPHTHENE DERIVATIVES. PART II. alpha-(2-THIONAPHTHENYLMERCAPTO)-PROPIONIC ACIDS AND SOME OF THEIR DERIVATIVES

The synthesis and principal properties of alpha-(2-thionaphthenylmercapto)-propionic acids as well as of some of their derivatives have been described.Racemic acid was resolved by crystallization of its diastereometric salts with optically active bases.The asymmetric transformation of laevorotatory alpha-bromopropionic acid to delta(+)alpha-(2-thionaphthenylmercapto)-propionic acid was carried out.The absolute configurations of the enantiomers were elucidated.Optical rotatory dispersion of the laevorotatory enantiomer and its p-bromophenacyl and p-phenylphenacyl esters in the region 365Safety of Benzo[b]thiophen-3(2H)-one

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Can You Really Do Chemisty Experiments About 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

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Synthesis of 3-[4-(2-aminoethoxy)-benzoyl]-2-aryl-6-hydroxy-benzo[B]thiophenes

The present invention is directed to chemical processes for preparing 2-aryl-6-hydroxy-3-[4-(2-aminoethoxyl)benzoyl]benzoyl]benzo[b]-thiophenes.

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Awesome and Easy Science Experiments about 5-Bromobenzothiophene

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Reference of 4923-87-9, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 4923-87-9, molcular formula is C8H5BrS, introducing its new discovery.

Modular Synthesis of Di- A nd Trisubstituted Imidazoles from Ketones and Aldehydes: A Route to Kinase Inhibitors

A one-pot and modular approach to the synthesis of 2,4(5)-disubstituted imidazoles was developed based on ketone oxidation, employing catalytic HBr and DMSO, followed by imidazole condensation with aldehydes. This methodology afforded twenty-nine disubstituted NH-imidazoles (23%-85% yield). A three-step synthesis of 20 kinase inhibitors was achieved by employing this oxidation-condensation protocol, followed by bromination and Suzuki coupling in the imidazole ring to yield trisubstituted NH-imidazoles (23%-69%, three steps). This approach was also employed in the synthesis of known inhibitor GSK3037619A.

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Simple exploration of Methyl benzo[b]thiophene-2-carboxylate

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Telomerase inhibitors

Methods and compositions for treating cancer and other diseases in which inhibition of telomerase activity can ameliorate disease symptoms or prevent or treat the disease relate to compounds characterized by the following structure: STR1 and their pharmaceutically acceptable salts. Y is selected from the group consisting of oxygen, sulfur, sulfonyl, sulfinyl, and –NR7 –. R1 is –TR8, where T is –C(X1)– or –SO2 –, and R8 is selected from the group consisting of –OR9, –NHNHSO2 R9, –NHNHC(X2)OR9, –NR9 R10, –NHNHC(X2)NR9 R10, –NHCR9 R10 C(X2)NR11 R12, –NHC(X2)NR9 R10, and the piperazinyl moiety shown below: STR2 where n is 0 or 1, and Qn, for n=1, is –SO2 –, –C(X2)– or –C(X2)NR10 –. R2 -R6 are selected independently from the group consisting of hydrogen, alkyl, aryl, hydroxyl, alkoxyl, aryloxyl, aralkoxyl, halogen, cyano, nitro, alkylcarbamido, arylcarbamido, dialkylcarbamido, diarylcarbamido, alkylarylcarbamido, alkylthiocarbamido, arylthiocarbamido, dialkylthiocarbamido, diarylthiocarbamido, alkylarylthiocarbamido, amino, alkylamino, arylamino, dialkylamino, diarylamino, arylalkylamino, aminocarbonyl, alkylaminocarbonyl, arylaminocarbonyl, dialkylaminocarbonyl, diarylaminocarbonyl, arylalkylaminocarbonyl, alkylcarbonyloxy, arylcarbonyloxy, carboxyl, alkoxycarbonyl, aryloxycarbonyl, sulfo, alkylsulfonylamido, arylsulfonylamido, alkylsulfonyl, arylsulfonyl, alkylsulfinyl, and arylsulfinyl. X1 and X2 are selected independently from the group consisting of oxygen, and sulfur. R7 -R12 are selected independently from the group consisting of hydrogen, alkyl, aryl, aralkyl, heterocycle, and heterocyclealkyl.

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New explortion of 2-Bromobenzo[b]thiophene

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Ruthenium-Catalyzed Direct and Selective C-H Cyanation of N-(Hetero)aryl-7-azaindoles

An efficient, highly regioselective, and scalable ruthenium-catalyzed o-aryl C-H mono-cyanation of N-aryl-7-azaindoles to form N-(2-cyanoaryl)-7-azaindoles has been developed through N-directed ortho C-H activation using N-cyano-N-phenyl-p-toluenesulfonamide as cyanating reagent in the presence of AgOTf and NaOAc in DCE. A range of substrates has furnished cyanated azaindoles in good to excellent yields under the simple reaction conditions. Involvement of C-H metalation has been supported by a kinetic study. This methodology provides easy access to a class of pharmaceutically significant molecules and their precursors.

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Brief introduction of 20503-40-6

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AMIDE COMPOUND

There is provided a FAAH inhibitor and a prophylactic or therapeutic agent for cerebrovascular disorders or sleep disorders comprising it. The prophylactic or therapeutic agent comprises a compound of the formula (I0): wherein Z is oxygen or sulfur; R1 is aryl which may be substituted, or a heterocyclic group which may be substituted; R1a is a hydrogen atom, a hydrocarbon group which may be substituted, hydroxyl, etc.; R2 is piperidin-1,4-diyl which may be substituted, or piperazin-1,4-diyl which may be substituted; R3 is a group formed by eliminating two hydrogen atoms from a 5-membered aromatic heterocyclic group having 1 to 3 heteroatoms selected from nitrogen, oxygen and sulfur, which may be further substituted, -CO-, etc.; and R4 is a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted; or a salt thereof.

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Awesome Chemistry Experiments For 5-Bromobenzothiophene

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NOVEL ANTHRANILIC ACID DERIVATIVE OR SALT THEREOF

The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula -X3-X4- or -X4-X3-, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP-13 production inhibitory effect.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem