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Radiolabelled raloxifene (LY156758) has been prepared by tritium gas hydrogenolysis of a 3-aroyl-bis-brominated precursor. The requisite halogenated intermediate was accessed by regioselective aroylation of benzothiophene 6 with the acid chloride of 3,5-dibromo-4-[2-(1-piperdinyl)ethoxy]benzoic acid (5). Selective deprotection of the aryl methyl ethers in the presence of the ethoxy side-chain followed by palladium catalyzed halogen-tritium exchange provided the target compound with a specific activity of 30.1 Ci/mmol.

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In chemical reaction engineering, simulations are useful for investigating and optimizing a particular reaction process or syste. Synthetic Route of 63675-74-1

The invention is a compound of Formula (I): whereinR is ?OH,R1 is ?OH,R2 is ?H,n is 2 or 3 andX is sulfur, ora pharmaceutically acceptable salt of a compound having Formula (1), ora pharmaceutical composition comprising a compound having Formula (1) or a pharmaceutically acceptable salt thereof, ormethods of treating bone loss, breast cancer or prostate cancer comprising administering an effective amount of the compound having Formula (I) or a pharmaceutically acceptable salt thereof.

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The present invention is directed to new processes for the synthesis of 2-aryl benzo[b]thiophenes.

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The present disclosure relates to compounds that act as antagonists via binding to the ER ligand binding domain non-covalently or covalently, or act as both antagonists and ER protein degraders, and the synthesis of the same. Further, the present disclosure teaches the utilization of such compounds in a treatment for proliferative diseases, including cancer, particularly breast cancer, and especially ER+ breast cancer.

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In an effort to develop novel affinity labeling agents for the estrogen receptor, we have synthesized two nonsteroidal ligands, a 1-aroyl-2-aryl tetralin system (1) and a 2-aryl-3-aroylbenzothiophene system (2).These agents, patterned after the Lilly antiestrogens trioxifene and LY 117018, respectively, embody acyl azide functions as part of a benzoyl chromophore.The acyl azide group has weak acylating activity, suitable for electrophilic affinity labeling,but this function is also photoreactive and, in its particular embodiment within these ligands, it could provide an efficient photochemical route to the highly reactive singlet acyl nitrene.The tetralin system (1) was prepared nine steps from 6-methoxy-1-tetralone, and the benzothiophene system (2) was prepared in four steps from a known substituted benzothiophene precursor.In competitive binding assays, both compounds show reasonable binding affinity for the rat and lamb uterine estrogen receptor : estradiol = 100percent, 1 = 3percent, and 2 = 12percent.When assayed by indirect receptor consumption assays, both compounds appear to have substantial capacity for irreversible binding (electrophilic reaction) with the receptor.This reactivity, which suggests that acylation of the receptor has occurred, is photoreversible.The nature of this ligand-receptor interaction is being investigated further. keywords: estrogen receptor, affinity labeling, photoaffinity labeling, nonsteroidal estrogens, antiestrogens, steroids

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Chemistry involves the study of all things chemical – chemical processes, chemical compositions and chemical manipulation – in order to better understand the way in which materials are structured, how they change and how they react in certain situations. name: 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

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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In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. The reactant in an enzyme-catalyzed reaction is called a substrate. Application In Synthesis of 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene, C16H14O2S. A document type is Patent, introducing its new discovery., Application In Synthesis of 6-Methoxy-2-(4-methoxyphenyl)-1-benzothiophene

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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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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The result showed that such a combination of chemo- and biocatalysis improved the catalytic yield more than two times compared with that of sole metal catalysis.I hope my blog about 63675-74-1 is helpful to your research.

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The instant invention provides an amorphous form of a compound of formula I. wherein: R1and R3are independently hydrogen, -CH3,-CO(C1-C6alkyl), or -COAr, wherein Ar is optionally substituted phenyl; R2is selected from the group consisting of pyrrolidinyl, hexamethyleneimino, and piperidinyl; or a pharmaceutically acceptable salt or solvate thereof. Methods of preparing the material, as well as methods of using same, are also provided.

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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