Article ID Journal Published Year Pages File Type
5279909 Tetrahedron Letters 2010 4 Pages PDF
Abstract

A formal total synthesis of the benzothiophene selective estrogen receptor modulator (SERM) desketoraloxifene and analogs has been accomplished from alkynes bearing electron-rich aromatic rings by electrophilic cyclization using I2. This approach affords oxygen-bearing 3-iodobenzo[b]thiophenes in excellent yields, which are easily further elaborated using a two-step approach involving Suzuki-Miyaura and Mitsunobu coupling reactions.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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