38567-00-9Relevant academic research and scientific papers
Synthesis and evaluation of raloxifene derivatives as a selective estrogen receptor down-regulator
Shoda, Takuji,Kato, Masashi,Fujisato, Takuma,Misawa, Takashi,Demizu, Yosuke,Inoue, Hideshi,Naito, Mikihiko,Kurihara, Masaaki
, p. 2914 - 2919 (2016)
Estrogen receptors (ERs) play a major role in the growth of human breast cancer cells. A selective estrogen receptor down-regulator (SERD) that acts as not only an inhibitor of ligand binding, but also induces the down-regulation of ER, would be useful fo
Piperidine nucleophilic substitution without solvent: An efficient synthesis of raloxifene
Yang, Yewei,Zhang, Tao,Huang, Wenhai,Shen, Zhenrong
, p. 3271 - 3276 (2014)
Mild and high-yielding synthesis is described for raloxifene via piperdine nucleophilic substitution of a new raloxifene intermediate 3-aroyl-2-aryl-substituted benzo[b]thiophenes, which is obtained by acylation of para-substituted benzoyl chlorides and 2-arylbenzo[b]thiophenes. The key step is solvent free and offers valuable advantages, such as low cost, and is suitable for industrial production.
Palladium catalyzed chloroethoxylation of aromatic and heteroaromatic chlorides: An orthogonal functionalization of a chloroethoxy linker
Petho, Bálint,Vangel, Dóra,Csenki, János T.,Zwillinger, Márton,Novák, Zoltán
supporting information, p. 4895 - 4899 (2018/07/15)
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.
Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists
Lemoine, Rémy C.,Petersen, Ann C.,Setti, Lina,Chen, Lijing,Wanner, Jutta,Jekle, Andreas,Heilek, Gabrielle,deRosier, André,Ji, Changhua,Rotstein, David M.
scheme or table, p. 1830 - 1833 (2010/07/02)
The bicyclic 5-amino-3-azabicyclo[3.3.0]octanes were shown to be effective replacements for the conformationally restricted 4-aminopiperidine ring found in several series of CCR5 antagonists.
Synthesis and preliminary use of novel acrylic ester-derived task-specific ionic liquids
Anjaiah, Siddam,Chandrasekhar, Srivari,Grée, René
, p. 569 - 571 (2007/10/03)
Novel electrophilic alkenes bearing an ionic liquid-type appendage have been prepared and used in Diels-Alder cycloadditions, 1,4-additions, Heck couplings and Stetter reactions; this new type of support allows easy monitoring of the reactions by NMR and MS as well as simple and efficient work-up and isolation procedures.
Benzothiophenes and related compounds as estrogen agonists
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Page/Page column 41-42, (2010/02/07)
The invention is a compound of Formula (I): wherein R is —OH, R1is —OH, R2is —H, n is 2 or 3 and X is sulfur, or a pharmaceutically acceptable salt of a compound having Formula (1), or a pharmaceutical composition comprising a compou
Processes for preparing benzothiophenes
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, (2008/06/13)
The present invention relates to intermediates and processes for preparing benzothiophenes.
Process for preparing benzothiophenes
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, (2008/06/13)
The present invention relates to intermediates and processes for preparing benzothiophenes of the following formula: wherein Y is chloro, bromo, iodo or -SO2R9; and, R9is C1-C4alkyl, trifluoromethyl,
Anti-arrhythmic agents
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, (2008/06/13)
A series of [N-alkyl-N-(nitro-, alkylsulphonamido, or amino-phenalkyl)amino]-alkyl, alkoxy or alkylthio phenyl derivatives having utility as anti-arrhythmic agents.
