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Regioselective alkylation process for preparing substituted benzo[b]thiophenes

The present invention provides processes for the regioselective alkylation of benzothiophenes.

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

 

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A Chimeric SERM-histone deacetylase inhibitor approach to breast cancer therapy

Breast cancer remains a significant cause of death in women, and few therapeutic options exist for estrogen receptor negative (ER (-)) cancers. Epigenetic reactivation of target genes using histone deacetylase (HDAC) inhibitors has been proposed in ER (-) cancers to resensitize to therapy using selective estrogen receptor modulators (SERMs) that are effective in ER (+) cancer treatment. Based upon preliminary studies in ER (+) and ER (-) breast cancer cells treated with combinations of HDAC inhibitors and SERMs, hybrid drugs, termed SERMostats, were designed with computational guidance. Assay for inhibition of four typea I HDAC isoforms and antagonism of estrogenic activity in two cell lines yielded a SERMostat with 1-3a muM potency across all targets. The superior hybrid caused significant cell death in ER (-) human breast cancer cells and elicited cell death at the same concentration as the parent SERM in combination treatment and at an earlier time point.

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

 

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Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo

The synthesis of benzothiophenes containing a piperazine side chain and their binding affinities for estrogen receptors are described. These compounds bearing piperazine side chains were identified to be high-affinity ligands with high selectivity for ER alpha subtype. They were also potent agonists in bone tissue.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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ANTIESTROGEN COMPOUNDS

A genus of proteolysis-targeting chimeras (PROTACs)-type compounds/antiestrogens has now been found that act as selective estrogen receptor degraders (SERDs) and estrogen receptor antagonists by degrading and antagonizing ERa in breast cancer cells. The compounds are of the following genus: The compounds described herein exhibit anti-proliferative effects, and are potentially useful, alone or in combination with other therapies, for the treatment of breast cancer. In general, these compounds combine a tight binding ERa targeting ligand tethered to a recognition motif or degron. Once bound, the degron recruits destructive cellular components and the targeted receptor (i.e., ERa) is degraded (i.e., destroyed) or antagonized.

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

 

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Benzothiophene compounds, intermediates, compositions, and method for inhibiting restenosis

The present invention provides pharmaceutically active compounds of formula I STR1 wherein R1 is –H, –OH, –O(C1 -C4 alkyl), –OCOC6 H5, –OCO(C1 -C6 alkyl), or –OSO2 (C2 -C6 alkyl); R2 is –H, –OH, –O(C1 -C4 alkyl), –OCOC6 H5, –OCO(C1 -C6 alkyl), –OSO2 (C2 -C6 alkyl), or halo, providing when Z is –S–, R2 is not halo; R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; and z is –O– or –S–; or a pharmaceutically acceptable salt thereof, for inhibiting restenosis.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Sulfur-alkyne cyclizations for formation of dihydrothiophenes and annulated thiophenes

Cycloisomerization of homopropargylic thiols to dihydrothiophenes is promoted by group VI metal carbonyls. Related thiacyclization transformations under basic and radical conditions are also described, including regioselective formation of benzothiophenes from aryl methyl sulfides and alkynes.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Demethylation process for preparing benzo[b]thiophenes

The preparation of benzo[b]thiophenes by the acylation of alkoxy protected starting materials followed by demethylation using essentially odorless thiol compound (2-methyl-5-t-butyl benzenethiol) are provided herewith. Demethylation may be carried out in the same reaction vessel without isolation of the acylated, protected material.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 63675-74-1, and how the biochemistry of the body works.Electric Literature of 63675-74-1

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An efficient one-pot synthesis of substituted 2-arylbenzo[b]thiophene derivatives

This communication describes an efficient one-pot procedure for the synthesis of 2-arylbenzo[b]thiophene derivatives via reaction of o-halo or nitro aryl carbonyl compounds with benzyl mercaptans in the presence of an excess of anhydrous K2CO3 at elevated temperature.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Balanced chemical reaction does not necessarily reveal either the individual elementary reactions by which a reaction occurs or its rate law.Synthetic Route of 63675-74-1. In my other articles, you can also check out more blogs about 63675-74-1

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A process for preparing benzo[b]thiophene derivatives

The present invention relates in general to the field of organic chemistry, and in particular to the preparation of benzo[b]thiophene derivatives. These benzo[b]thiophene derivatives are useful as intermediates in the synthesis of pharmaceutically active agents such as raloxifene or derivatives thereof.

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

 

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2-arylbenzo[B]thiophenes useful for the treatment of estrogen deprivation syndrome

This invention provides methods which are useful for the inhibition of the various medical conditions associated with estrogen deprivation syndrome including osteoporosis and hyperlipidemia utilizing compounds of formula I: STR1

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