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Zindoxifene, NSC-341952, D-16726

秦哚昔芬Chemical Name: 5-Acetoxy-2-(4-acetoxyphenyl)-1-ethyl-3-methylindole
CAS No. 86111-26-4
项目整合开发状态: Phase II
项目研究机构: Degussa (Originator)
合成路线:4-Methoxyaniline (I) is reacted with 2'-bromo-4-methoxypropiophenone (II) to afford the indole (III).The ethyl group is introduced by deprotonation with sodium hydride in DMF followed by addition of ethyl bromide.The ether cleavage of (IV) with BBr3 yields the hydroxy derivative (V),which is converted to the acetate by using acetic acid an hydride in pyridine.
📌 参考资料/链接:
参考文献标题:D-16726
文献作者:von Angerer,E.; Sheldrick,W.S.; Engel,J.; Schneider,M.R.
参考来源:Drugs Fut 1985,10(4),281

📄 详细内容


合成路线:4-Methoxyaniline (I) is reacted with 2'-bromo-4-methoxypropiophenone (II) to afford the indole (III).The ethyl group is introduced by deprotonation with sodium hydride in DMF followed by addition of ethyl bromide.The ether cleavage of (IV) with BBr3 yields the hydroxy derivative (V),which is converted to the acetate by using acetic acid an hydride in pyridine.
参考文献标题:Benzo[a]carbazole derivatives.Synthesis,estrogen receptor binding affinities,and mammary tumor inhibiting activity
文献作者:von Angerer,E.; Prekajac,J.
参考来源:J Med Chem 1986,29(3),380-6


产品链接: CAS No. 86111-26-4››