Piperidine Nucleophilic Substitution Without Solvent: An Efficient Synthesis of Raloxifene |
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| Authors: | Yewei Yang Tao Zhang Wenhai Huang |
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| Affiliation: | Zhejiang Academy of Medical Sciences , Hangzhou , China |
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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. |
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| Keywords: | Friedel–Crafts acylation green chemistry nucleophiles raloxifene SERM |
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