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Visible light photocatalytic synthesis of benzothiophenes

The photocatalytic reaction of o-methylthio-arenediazonium salts with alkynes yields substituted benzothiophenes regioselectively through a radical annulation process. Green light irradiation of eosin Y initiates the photoredox catalysis. The scope of the reaction was investigated by using various substituted diazonium salts and different alkynes.

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Benzothiophene – Wikipedia,
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Description anti-mitotic agents which inhibit tubulin polymerization

Methoxy and ethoxy substituted 3-aroyl-2-arylbenzo[b]thiophenes and benzo[b]thiophene analogues are described for use in inhibiting tubulin polymerization. The compounds’ use for treating tumor cells is also described. Additional aspects described here are certain diaryl ether benzo[b]thiophene derivatives. Also described are particular analogs derived from dihydronaphthalene which have proven particularly effective. Certain new benzofuran analogs are described, as well as certain sulfur oxide benzo[b]thiophene analogs. Important compounds described herein include the first nitrogen-containing derivatives of combretastatin. These include nitro, amino and azide combrdtastatin derivatives.

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Benzothiophene – Wikipedia,
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2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents

Derivatives of 2-phenyl-3-aroylbenzothiophenes and 2-phenyl-3-aroylbenzothiophene-1-oxides are useful as antifertility agents. Certain of these compounds also are useful in suppressing the growth of mammary tumors.

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Benzothiophene – Wikipedia,
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ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS

The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

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Reference£º
Benzothiophene – Wikipedia,
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Benzothiophenes, and formulations and methods using same

The present invention provides a class of substituted benzo[ b] thiophene compounds of the structure and pharmaceutical compositions comprising the compounds useful, either alone or in combination with estrogen or progestin, in the symptomatic treatment of post-menopausal syndrome, particularly osteoporosis, cardiovascular related pathological conditions, and estrogen-dependent cancer.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Benzothiophene compounds, intermediates, compositions, and methods

The present invention provides a method for inhibiting endometriosis comprising administering to a woman an effective amount of a compound of formula I STR1 wherein R1a is –H or –OR7a in which R7a is –H or a hydroxy protecting group; R2a is –H, halo, or –OR8a in which R8a is –H or a hydroxy protecting group; R3 is 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 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.

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Benzothiophene – Wikipedia,
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Preparation of Benzothiophenes and Benzoselenophenes from Arylamines and Alkynes via Radical Cascade Reactions

An intermolecular radical cascade reaction between readily prepared o-methylthio-arylamines or o-methylselanyl-arylamines and alkynes for the preparation of valuable benzothiophenes or benzoselenophenes is reported. These transformations occur efficiently with complete regioselectivity and the products are obtained in moderate to good yields. The current protocol is successfully applied to the synthesis of the key intermediates of the drug raloxifene and an AT1receptor antagonist.

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Benzothiophene – Wikipedia,
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Nucleophilic aromatic substitution on 3-aroyl-2-arylbenzothiophenes. Rapid access to raloxifene and other selective estrogen receptor modulators

Versatile, mild and high yielding methods for nucleophilic aromatic substitution of 2-dialkylamino-1-ethoxides and related nucleophiles on 3- aroyl-2-arylbenzothiophene nuclei are presented. A short synthesis of raloxifene is detailed.

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Benzothiophene – Wikipedia,
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Toward selective ERbeta agonists for central nervous system disorders: Synthesis and characterization of aryl benzthiophenes

In an effort to identify selective for the estrogen receptor subtype ERbeta, a series of aryl benzthiophenes was synthesized. In a radioligand binding assay and reporter gene assat in HeLa and SH-SY5Y cells, compound were characterized as ERbeta-selective agonists. By targeting ERbeta in the brain, these compounds could lead to drugs able to separate the beneficial effects of estrogens on mood, learning, and memory from side effects such as the stimulation of edometrial and breast cancer.

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Benzothiophene – Wikipedia,
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Benzothiophene compounds, compositions, and method

The invention provides benzothiophene compounds, formulations, and methods of inhibiting bone loss or bone resorption, particularly osteoporosis, and cardiovascular-related pathological conditions including hyperlipidemia, and estrogen-dependent cancer.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem