含Cyclofenil结构单元的三羰基铼配合物的合成.pdfVIP

2009 年第 29 卷 有 机 化 学 Vol. 29, 2009 第 9 期, 1450～1456 Chinese Journal of Organic Chemistry No. 9, 1450～1456 ·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 (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) 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 [Et N] [Re(CO) Br ]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 4 2 3 3 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 Synthesis of Cyclofenil Rhenium Tricarbonyl Conjugates Zhu, Huaa,b Huang, Lilianga,b Zhang, Chunchuna,b Xu, Jiaa Shen, Yumei*,a 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 nu- cleophilic substitution. The study provides a useful assessment of the stage of the breast cancer by imaging ERβ with the SPECT (single photon emis