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A series of benzoyl and cinnamoyl nitrogen mustards tethered to different benzoheterocycles and to oligopyrroles structurally related to netropsin consisting of two pyrrole-amide units and terminating with an amidine moiety have been synthesised and a structure-activity relationship determined. Derivatives 3-10 have been evaluated for their sequence selective alkylating properties and cytotoxicity against human K562 leukaemia cells. They are 2- to 50-fold less cytotoxic than tallimustine, with compound 8 being the most potent member of this series. Among tallimustine isosters, the compounds with an indole 3 or benzothiophene 6 are 4-fold less cytotoxic than tallimustine, while the compounds with an N-methyl indole or benzofuran showed a 7- and 14-fold reduced cytotoxic potency, respectively. Our preliminary results indicate that these derivatives preferentially bind to AT-rich sequence with a sequence selectivity similar to tallimustine.

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Reference:
Benzothiophene – Wikipedia,
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The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formulae (I), (II) and (III). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

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Benzothiophene – Wikipedia,
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A new synthetic method for dimethyl 2,3-dihydrobenzo[b]oxepine-2,4- dicarboxylates and methyl 2-(2- carbomethoxybenzo[b]furan-3-yl)propanoates by an intramolecular conjugate displacement reaction or an SN2 reaction of acetates of Morita-Baylis-Hillman adducts of methyl (2-formylphenoxy)acetates has been described.

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Reference:
Benzothiophene – Wikipedia,
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The present invention provides an improved process for the preparation of alpha-(3- methoxyphenylthio)-4-methoxyacetophenone. The present invention also provides a process for the preparing free flowing solid of 6-methoxy-2-(4-methoxyphenyl)- benzo[b]-thiophene. The present invention further provides a process for the preparation of substantially pure 6-methoxy-2-(4-methoxyphenyl)-benzo[b]-thiophene. The present invention further provides a process for purification of raloxifene hydrochloride.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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New Advances in Chemical Research in 2021. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction by binding to a specific portion of an enzyme and thus slowing or preventing a reaction from occurring. Application In Synthesis of 2-(5-Bromo-2-fluorobenzyl)benzo[b]thiophene, In an article, mentioned the application of 1034305-17-3, Name is 2-(5-Bromo-2-fluorobenzyl)benzo[b]thiophene, molecular formula is C15H10BrFS

The present invention provides a method for synthesizing geleg only Iraq, the prepared composite organic metal reagent with 2 – (5-bromo-2-fluorobenzyl) benzothiophene halogen exchange to obtain the aryl metal compound intermediate; aryl metal compound occurs with gluconic acid lactone intermediates for the coupling reaction, hydroxy protection by dehydration 1-C – [3 – (benzo [B] thiophene-2-yl methyl) – 4-fluoro phenyl]-ALPHA-D-pyran glucitol; 1-C – [3 – (benzo [B] thiophene-2-yl methyl) – 4-fluoro phenyl]-ALPHA-D-pyran anhydroglucitol crude product obtained after reduction of net iraqi Geleg ; iraqi Geleg net crude purified acylated, and net iraqi Geleg deacyl reaction to obtain pure product. The composite organic metal reagent, the reaction temperature is increased, the cost is saved, is suitable for industrial production; the protection of the dehydroxylated aqueous acid, the crude product is solid and non-oil material, it is convenient to process and shorten the reaction time. (by machine translation)

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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The invention relates to novel 2-heteroaryl carboxamides and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.

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The invention belongs to the field of polymer technology, discloses a based on the fused ring furan small molecule material preparation method and its application, including: to 2, 3 – dibromo furan, 2, 3 – dibromo thiophene, 2, 3 – two bromine selenophens, 2, 3 – dibromo – indole derivatives and 2 – hydroxybenzene acid derivatives as raw materials, through the Suzuki reaction to obtain the key intermediate; to cuprous or copper compound as catalyst, 1, 10 – phenanthrene or bipyridyl compound is a ligand, molecule in Ullman C – O coupling reaction, synthesizing a series of fused ring furan small molecule material. The substrates of the invention synthesis is relatively simple, high yield; furan ring reaction time is greatly shortened; cuprous compound and compound bipyridine catalysis system cheaper; mild reaction condition; substrate and wide range of application; the reaction yield is high, can be as high as 97%. Therefore the method is suitable for industrial production. (by machine translation)

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Benzothiophene – Wikipedia,
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Modular conditions for the formation of thioureas or pyrimidine-4-one-2- thiones connected to the benzo[b]thiophene, benzene and indole structures were performed. A benzo[b]thiophene isothiocyanate derivative was used as a model to study the condensation with simple aromatic amines and amino-l-sorbose derivative. The construction of pyrimidine-4-one-2-thiones using basic conditions afforded efficiently new heterocyclic aromatics, which were further transformed using the alkylated sulfur as a leaving group in palladium-catalyzed cross-coupling reactions.

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Reference:
Benzothiophene – Wikipedia,
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A series of terarylenes incorporating benzothiophene (BT)/benzofuran (BF) as the central ethene unit was synthesised by using sequential Pd-catalysed C – H activation reactions. This new methodology allows the easy modification of the nature of the pendant heteroarene groups. Diaryl ethene (DAE) derivatives with thiophene, thiazole, pyrrole, isoxazole and pyrazole rings were prepared. A large number of asymmetrical DAEs are easily accessible by this new method in both the BT and BF series. The study of their photochromic properties in solution revealed that the nature of the heteroarene and of the central unit drastically modify their photochromic behaviour. TD-DFT calculations were performed to assess the nature of the relevant excited states.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Anodic fluorination of benzo[b]thiophene derivatives provided a complex mixture of di- and trifluorinated products. On the other hand, anodic fluorination of 3-oxo-2,3-dihydrobenzo[b]thiophene and methyl 3-oxo-2,3-dihydrobenzo[b]thiophene-2-carboxylate gave the corresponding monofluorinated products selectively in moderate yields. Anodic fluorination of methyl alpha-(2-cyanophenylthio)acetate followed by intramolecular cyclization provided 3-amino-2-fluorobenzo[b]thiophene in excellent yield. Georg Thieme Verlag Stuttgart · New York.

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Reference:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem