Piperidine Nucleophilic Substitution Without Solvent: An Efficient Synthesis of Raloxifene |
| |
| Authors: | Yewei Yang Tao Zhang Wenhai Huang |
| |
| Institution: | Zhejiang Academy of Medical Sciences , Hangzhou , China |
| |
| Abstract: | Mild and high-yielding synthesis is described for raloxifene via piperdine nucleophilic substitution of a new raloxifene intermediate 3-aroyl-2-aryl-substituted benzob]thiophenes, which is obtained by acylation of para-substituted benzoyl chlorides and 2-arylbenzob]thiophenes. The key step is solvent free and offers valuable advantages, such as low cost, and is suitable for industrial production. |
| |
| Keywords: | Friedel–Crafts acylation green chemistry nucleophiles raloxifene SERM |
|
