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有机化学
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有机化学 ›› 2009, Vol. 29 ›› Issue (9): 1450-1456. 上一篇    下一篇

研究简报

含Cyclofenil结构单元的三羰基铼配合物的合成

朱 华a,b 黄立梁a,b 张春春a,b 许 嘉a 沈玉梅*,a   

  1. (a中国科学院上海应用物理研究所放射性药物研究中心 上海 201800)
    (b中国科学院研究生院 北京 100049)
  • 收稿日期:2008-09-27 修回日期:2009-03-09 发布日期:2009-12-30
  • 通讯作者: 沈玉梅

Synthesis of Cyclofenil Rhenium Tricarbonyl Conjugates

Zhu, Huaa,b Huang, Lilianga,b Zhang, Chunchuna,b Xu, Jiaa Shen, Yumei*,a   

  1. (a Research Center of Radiopharmaceuticals, Shanghai Institute of Applied Physics, Chinese Academy of Sciences,
    Shanghai 201800)
    (b Graduate School of the Chinese Academy of Sciences, Beijing 100049)
  • Received:2008-09-27 Revised:2009-03-09 Published:2009-12-30
  • Contact: Shen, Yumei

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被引次数

3 | 2

以4,4’-二羟基二苯甲酮为原料, 通过McMurry反应合成了三种环芬尼类化合物. 优化条件实现两个酚羟基选择性生成单ω-溴代烷基醚, 通过亲核取代反应连接三齿螯合剂, 得到了一系列雌激素受体β分子探针前体. 用[Et4N]2[Re(CO)3Br3]与之配位合成了其冷标记配合物, 为SPECT (single photon emission computed tomography)显像雌激素受体β从而评估乳腺癌的恶化程度奠定了基础. 产物通过IR, 1H NMR, 13C NMR, HRMS或元素分析进行了表征.

关键词: 环芬尼, 三羰基铼, 乳腺癌

Starting from 4,4’-dihydroxybenzophenone, three kinds of cyclofenil analogues were prepared by Mcmurry coupling. Under optimized conditions a series of cyclofenil rhenium(I) tricarbonyl conjugates were prepared as molecular probe precursors of estrogen receptor β by ω-bromoalkylation and subsequent nucleophilic substitution. The study provides a useful assessment of the stage of the breast cancer by imaging ERβ with the SPECT (single photon emission computed tomography) technique. The structures of final products and the intermediates were confirmed by IR, 1H NMR, 13C NMR, HRMS techniques or elemental analysis.

Key words: rhenium tricarbonyl, breast cancer, cyclofenil