An Expeditious Synthesis of Lasofoxifene and Nafoxidine via the Novel Three-component Coupling Reaction
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The simple and efficient synthesis of lasofoxifene (<B>4</B>), a possible candidate for alleviating osteoporosis, via the novel three-component coupling reaction among 4-pivaloyloxybenzaldehyde (<B>5</B>), cinnamyltrimethylsilane (<B>6</B>), and anisole in the presence of HfCl<SUB>4</SUB> is illustrated. The successive cationic cyclization of the coupling product, olefin formation, and migration of the double-bond are performed to afford the common synthetic intermediate of lasofoxifene (<B>4</B>) and nafoxidine (<B>3</B>) via a very concise procedure.
- Chemistry Letters
Chemistry Letters 36(1), 40-41, 2007-01-05
The Chemical Society of Japan