Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5279909 | Tetrahedron Letters | 2010 | 4 Pages |
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.
Graphical abstractDownload full-size image
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Chul-Hee Cho, Dai-Il Jung, Richard C. Larock,