Discovery of 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

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.Formula: C16H14O2S

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 63675-74-1, name is 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene, introducing its new discovery. Formula: C16H14O2S

Compounds with hydroxycarbonyl-halogenoalkyl side chain

The present invention provides a compound consisting of a moiety and a group chemically bonded to said moiety, wherein said moiety contains a compound having low activity following oral administration or its parent scaffold and said group has the following general formula (1): 1in which R1 represents a hydrogen atom, etc., R2 represents a C1-C7 halogenoalkyl group, etc., m represents an integer of 2 to 14, and n represents an integer of 2 to 7, or enantiomers of the compound, or hydrates or pharmaceutically acceptable salts of the compound or enantiomers thereof. The above compound is advantageous in pharmaceutical use because the group of general formula (1) allows compounds such as anti-estrogenic ones to show a significantly increased activity following oral administration when attached to the parent scaffolds of the compounds.

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.Formula: C16H14O2S

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

 

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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 compounds 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,
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Process for preparing benzoic acid derivative intermediates and benzothiophene pharmaceutical agents

Novel processes for producing compounds of formula I STR1 wherein R1 and R2 each are independently C1 -C4 alkyl, or combine to form piperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; and n is 2 or 3; or a pharmaceutically acceptable salt thereof employing alkylacetate solvents are provided.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Substituted benzo(b)thiophene compounds having activity as selective estrogen receptor modulators

The present invention provides compounds with nitrogen, sulfur or carbon linked basic side chains of formula where R1and R2are independently hydrogen, halo, hydroxy, alkoxy, alkylcarbonyloxy, alkoxycarbonyl, alkoxycarbonyloxy, arylcarbonyloxy, aryloxycarbonyloxy, or alkylsulfonyloxy; O-SO2-(C4-C6alkyl), chloro, fluoro, or bromo; W is CHOH, C(O), or CH2; Y is -CH2-, -NH-, -NMe-, -S-, -SO2-; and R3and R4are independently hydrogen, alkyl, alkylcarbonyl, alkylamino-carbonyl, or arylcarbonyl, or together with the nitrogen to which they are attached form 1-pyrrolidinyl, 1-piperidinyl, or a 5- or 6-membered imide or cyclic amide ring. The present invention also provides pharmaceutical compositions containing the compounds optionally containing estrogen or progestin, and the use of such compounds, alone, or in combination with estrogen or progestin, for treating osteoporosis, aortal smooth muscle cell proliferation, (particularly restenosis), and estrogen-dependent cancer (particularly breast cancer).

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

A new application about 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

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Synthetic Route of 63675-74-1, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.63675-74-1, Name is 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene, molecular formula is C16H14O2S. In a Patent£¬once mentioned of 63675-74-1

PROCESS FOR THE PREPARATION OF RALOXIFENE HYDROCHLORIDE

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£º
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Chapter 5: Synthesis of Raloxifene

Use of hazardous reagents is common in most of the reported synthesis of molecules of various interests. Hazardous reagents at a manufacturing scale pose a great challenge in terms of handling, operation and workups. These reagents are unsafe and found to have proven toxicity (in the majority of the cases). If not avoided, these reagents will defy the purpose of Green Chemistry and sustainability in organic synthesis. In this chapter, the synthesis of raloxifene, [6-Hydroxy-2-(4-hydroxyphenyl)-1-benzothiophen-3-yl]{4-[2-(piperidin-1-yl)eth-oxy] phenyl}methanone hydrochloride 1, an estrogen agonist/antagonist commonly considered as a selective estrogen receptor modulator (SERM), will be discussed considering the evolving trends of switching the usage of hazardous to less hazardous reagents. Raloxifene impedes the re-sorption of bone by reducing the biochemical markers of bone turnover in the premenopausal women thereby helping in the management of osteoporasis. Raloxifene hydrochloride also lowers the chances of developing a certain type of breast cancer (invasive breast cancer) in post-menopausal women.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

Brief introduction of 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

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Palladium catalyzed chloroethoxylation of aromatic and heteroaromatic chlorides: An orthogonal functionalization of a chloroethoxy linker

A novel disconnection based on cross-coupling chemistry was designed to access pharmaceutically relevant aryl-aminoethyl ethers. The developed palladium-catalyzed functionalization of aryl- and heteroaryl chlorides with a sodium tetrakis-(2-chloroethoxy) borate salt is orthogonal to the simple nucleophilic replacement of the chloro function of the ethylene linker. The transformation enables efficient 2-chloroethoxylation in the absence of an additional external base. Subsequent amine substitution of the alkyl halide affords 2-aminoethoxy arenes. The applicability of this method was demonstrated through the synthesis of various aryl- and heteroaryl-alkyl ethers, including the intermediates of marketed drug molecules.

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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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Synthesis of a Tetrafluoro-Substituted Aryl Azide and Its Protio Analogue as Photoaffinity Labeling Reagents for the Estrogen Receptor

A tetrafluoro-substituted aryl azide 1 and its protio analogue 2, both photoaffinity labeling reagents for the estrogen receptor, have been prepared by direct coupling of the appropriately substituted 4-azidobenzoyl chloride with the electron rich C-3 of 6-methoxy-2-(4-methoxyphenyl)benzothiophene 3.This represents a rare example of aryl azide stability under Friedel-Crafts acylation conditions.Alternatively, the protio analogue 2 can also be prepared with the azide functionality masked as a phthaloyl-protected arylamine, and the tetrafluoro analogue 1, by direct displacement of a pentafluoroaryl derivative 20 with NaN3.Solution photolysis of tetrafluoro-substituted aryl azide (bis-methyl ether) 15 and its protio analogue 16 in toluene at 30 deg C results in relatively high yields of products derived from C-H insertion.Both azides 1 and 2 demonstrate favorable relative binding affinity (RBA) (1 = 10percent, 2 = 66percent, estradiol = 100percent) and photoinactivation efficiency (1 = 43percent, 2 = 55percent at 30 min) for the estrogen receptor (ER).The synthesis of both azides has been modified to accommodate a palladium-catalyzed tritium gas hydrogenolysis of an iodoaryl precursor at a late stage in the synthetic sequence, as will be needed to prepare them in radiolabeled form, and this procedure has been verified dy deuteration.This pair of compounds will allow a detailed evaluation of the role that fluorine substitution plays in the photochemistry and photocovalent attachment behavior of aryl azides in a complex biochemical system, the estrogen receptor.The radiosynthesis and further biochemical results will be presented elsewhere.

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

 

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BENZOTHIOPHENE DERIVATIVES AS ESTROGEN RECEPTOR INHIBITORS

A compound of formula (I), or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem

 

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Two-Step Synthesis of Unsymmetrical Diaryl Sulfides by Electrophilic Thiolation of Non-functionalized (Hetero)arenes

This article reports the efficient preparation of a series of unsymmetrically substituted thioethers through a two-step procedure consisting of an initial metal-free C?H sulfenylation of electron-rich (hetero)arenes with newly prepared succinylthioimidazolium salts. Subsequent reaction of the arylthioimidazolium intermediates with Grignard reagents afford the desired thioethers. The synthetic protocol described is modular, scalable, and high yielding, and provides access to sulfides that are not easy to obtain through the existing methodologies. Importantly, no prefunctionalization of the initial (hetero)arene is required.

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Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem