铜介导的芳基硼前体的亲核放射性溴化反应：放射性溴化PARP-1抑制剂的便捷制备方法
Copper-Mediated Nucleophilic Radiobromination of Aryl Boron Precursors: Convenient Preparation of a Radiobrominated PARP-1 Inhibitor.
作者信息
Zhou Dong, Chu Wenhua, Voller Thomas, Katzenellenbogen John A
机构信息
Department of Radiology, School of Medicine, Washington University in Saint Louis, Saint Louis, MO 63110.
Department of Chemistry, University of Illinois at Urbana-Champaign, Urbana, IL 61801.
出版信息
Tetrahedron Lett. 2018 May 16;59(20):1963-1967. doi: 10.1016/j.tetlet.2018.04.024. Epub 2018 Apr 11.
Abstract
The copper-mediated nucleophilic radiobromination of aryl boron precursors with a radiobromide ion is a novel radiolabeling method that is efficient and robust. High radiochemical conversion (RCC) was observed using a variety of solvents, temperatures and catalysts. The reaction is also clean and is feasible for purification to obtain high chemical and radiochemical purity. This method provides a very useful route for the preparation of radiobrominated pharmaceuticals, including a radiobromine labeled PARP-1 inhibitor, and it is a valuable addition to the family of copper-mediated radiolabeling processes.
摘要
铜介导的芳基硼前体与放射性溴离子的亲核放射性溴化反应是一种高效且稳健的新型放射性标记方法。使用多种溶剂、温度和催化剂时均观察到了高放射化学转化率（RCC）。该反应也很纯净，对于纯化以获得高化学纯度和放射化学纯度是可行的。此方法为制备放射性溴化药物提供了一条非常有用的途径，包括一种放射性溴标记的PARP-1抑制剂，并且它是铜介导的放射性标记方法家族中的一个有价值的补充。
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