1-<4-(acetylamino)phenyl>-1-<4-<2-(N,N-dimethylamino)ethoxy>phenyl>-2-phenyl-1-butene | 97732-66-6

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 二苯乙烯类
• 英文名称: 1-<4-(acetylamino)phenyl>-1-<4-<2-(N,N-dimethylamino)ethoxy>phenyl>-2-phenyl-1-butene
• CAS: 97732-66-6
• 化学式: C₂₈H₃₂N₂O₂
• 分子量: 428.574
• InChiKey: WDIKOCNCPMBIMC-UHFFFAOYSA-N

反应信息

• 作为反应物：
  描述：

  1-<4-(acetylamino)phenyl>-1-<4-<2-(N,N-dimethylamino)ethoxy>phenyl>-2-phenyl-1-butene 在 盐酸 作用下， 以 甲醇 为溶剂， 反应 1.5h， 生成 (E)-1-(4-aminophenyl)-1-<4-<2-(N,N-dimethylamino)ethoxy>phenyl>-2-phenyl-1-butene 、 (Z)-1-(4-aminophenyl)-1-<4-<2-(N,N-dimethylamino)ethoxy>phenyl>-2-phenyl-1-butene
  参考文献：
  名称：

  Synthesis and receptor-binding affinity of fluorotamoxifen, a possible estrogen-receptor imaging agent

  摘要：

  Aminotamoxifen was totally synthesized from p-nitrobenzoyl chloride via a Friedel-Crafts acylation. Then, by means of a Balz-Schiemann reaction, aminotamoxifen was converted into fluorotamoxifen. The triazene variation of this conversion, with a 25% yield, enables a rapid, one-step diazotization, incorporating a fluorine atom into the phenyl ring of the tamoxifen. This reaction may be useful for the preparation of low specific activity 18F-labeled tamoxifen, for distribution, and for estrogen-receptor studies. For these in vivo and in vitro studies, fluorotamoxifen was also synthesized from p-fluorobenzoyl chloride, and its chemical intermediates were compared with estradiol and hexestrol, for their receptor binding and competition, as well as for their uterotropic activity. It is demonstrated that tamoxifen and fluorotamoxifen are strong estradiol agonists and partial hexestrol agonists, while aminotamoxifen is a weak estradiol and hexestrol agonist.

  DOI：

  10.1021/jm00148a022