Bromination of 3-substituted benzo[b]thiophenes: access to Raloxifen intermediate

详细信息    查看全文

• 作者：Franç ; ois Liger^a ; Sté ; phane Pellet-Rostaing ; ^a ; ^{stephane.pellet-rostaing@cea.fr"" rel=""nofollow} ; Florence Popowycz^a ; Marc Lemaire ; ^a ; ^{marc.lemaire@univ-lyon1.fr"" rel=""nofollow}
• 关键词：Benzo[b]thiophene ; Bromination ; Electrophilic aromatic substitution ; Raloxifen
• 刊名：Tetrahedron Letters
• 出版年：2011
• 出版时间：20 July 2011
• 年：2011
• 卷：52
• 期：29
• 页码：3736-3739
• 全文大小：514 K

文摘

A practical route to prepare halogeno-derivatives is described, starting from easily available 3-cyano-benzo[b]thiophene. Main efforts have been devoted to the optimization of the experimental procedures (solvent, bromination) to promote selectivity. Synthetic studies investigate the potential access to an advanced intermediate of Raloxifen.