103808-68-0Relevant academic research and scientific papers
Efficient synthesis of 3-benzoyl Benzo[b]thiophenes and raloxifene via Mercury(II)-Catalyzed cyclization of 2-alkynylphenyl alkyl sulfoxides
Wen, Shi-Ming,Lin, Cheng-Han,Chen, Chin-Chau,Wu, Ming-Jung
, p. 2493 - 2499 (2018/04/16)
The unique selective estrogen receptor modulator, Raloxifene (1), and antitubulin agent 2 were synthesized through the key intermediate, 4-methoxybenzyl 2-bromo-4-methoxyphenyl sulfoxide (6), respectively. It was found that compared with the o-sulfanyl aryl bromides, the sulfinyl group at ortho position accelerated the Sonogashira coupling reaction of aryl bromides. Thus, compound 6 was coupled with 3,4,5-trimethoxyphenyl acetylene, followed by mercury-catalyzed cyclization reaction afford compound 2 in 79% overall yield. Raloxifene (1) was prepared from compound 6 in four steps and 33% overall yield via coupling reaction with 1-trimethylsily-2-(4-tert-butyldimethylsiloxy)phenylethyne, mercury-catalyzed cyclization reaction, alkylation and demethylation.
Synthesis and growth inhibition activity of fluorinated derivatives of tamoxifen
Malo-Forest, Bianca,Landelle, Grégory,Roy, Jessye-Ann,Lacroix, Jacques,Gaudreault, René C.,Paquin, Jean-Fran?ois
, p. 1712 - 1715 (2013/03/29)
The design and synthesis of 11 fluorinated derivatives of tamoxifen are described. Growth inhibition values (GI50) on human HT-29, M21, MCF7, and MDA-MB-231 tumor cells are also reported. In general, the GI50 values are similar or sl
COMPOUNDS COMPRISING A LACTAM OR A LACTAM DERIVATIVE MOIETY, PROCESSES FOR MAKING THEM, AND THEIR USES
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Page/Page column 67, (2008/06/13)
The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.
Synthesis of tetracyclic heterocompounds as selective estrogen receptor modulators. Part 1. Process development for scale-up of 2,5,8-substituted 5,11 -dihydrochromeno[4,3-c]chromene derivatives
Li, Xun,Reuman, Michael,Russell, Ronald K.,Adams, Richard,Ma, Robert,Beish, Sandra,Branum, Shawn,Youells, Scott,Roberts, Jerry,Jain, Nareshkumar,Kanojia, Ramesh,Sui, Zhihua
, p. 414 - 421 (2012/12/31)
Unsymmetrical benzopyranobenzopyran compounds are novel selective estrogen receptor modulators (SERMs). A reproducible and nonchromatographic process was developed to prepare multihundred gram quantities of 5-(4-(2-(piperidin-1-yl) ethoxy)-phenyl)-5,11-di
