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Synthetic Communications
An International Journal for Rapid Communication of Synthetic Organic Chemistry
Volume 44, 2014 - Issue 22
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Original Articles

Piperidine Nucleophilic Substitution Without Solvent: An Efficient Synthesis of Raloxifene

Yewei Yang Zhejiang Academy of Medical Sciences, Hangzhou, China
,
Tao Zhang Zhejiang Academy of Medical Sciences, Hangzhou, China
,
Wenhai Huang Zhejiang Academy of Medical Sciences, Hangzhou, China
&
Zhenrong Shen Zhejiang Academy of Medical Sciences, Hangzhou, ChinaCorrespondence[email protected]
Pages 3271-3276 | Received 08 May 2014, Published online: 05 Sep 2014
 
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Abstract

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.

GRAPHICAL ABSTRACT

Notes

Color versions of one or more of the figures in the article can be found online at www.tandfonline.com/lsyc.

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