Short-step synthesis of droloxifene via the three-component coupling reaction among aromatic aldehyde, Cinnamyltrimethylsilane (cas 19752-23-9), and β-chlorophenetole

Add time:09/03/2019    Source:sciencedirect.com

A short-step route for the preparation of droloxifene has been established via the novel three-component coupling reaction among 3-pivaloyloxybenzaldehyde, cinnamyltrimethylsilane, and β-chlorophenetole, the successive installation of the side-chain part, and the base-induced migration of the double bond. The present synthesis of tetra-substituted ethylene moieties is a widely applicable strategy for producing a variety of SERMs (selective estrogen receptor modulators) and SARMs (selective androgen receptor modulators), such as tamoxifen, raloxifene, and other compounds that can lead to new drugs.

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