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| 含Cyclofenil结构单元的三羰基铼配合物的合成 | |
| 引用本文： | 朱华,黄立梁,张春春,许嘉,沈玉梅. 含Cyclofenil结构单元的三羰基铼配合物的合成[J]. 有机化学, 2009, 29(9): 1450-1456 |
| 作者姓名： | 朱华 黄立梁 张春春 许嘉 沈玉梅 |
| 作者单位： | 1. 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;中国科学院研究生院,北京,100049 2. 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 |
| 基金项目： | 中国科学院"百人计划"，中国科学院前沿领域 |
| 摘 要： | 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 |
| 收稿时间： | 2008-09-27 |
| 修稿时间： | 2009-03-09 |
Synthesis of Cyclofenil Rhenium Tricarbonyl Conjugates |
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| Zhu Hu,Huang Liliang,Zhang Chunchun,Xu Jia,Shen Yumei. Synthesis of Cyclofenil Rhenium Tricarbonyl Conjugates[J]. Chinese Journal of Organic Chemistry, 2009, 29(9): 1450-1456 | |
| Authors: | Zhu Hu Huang Liliang Zhang Chunchun Xu Jia Shen Yumei |
| Affiliation: | (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) |
| Abstract: | 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. |
| Keywords: | cyclofenil rhenium tricarbonyl breast cancer |
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