当前位置: X-MOL 学术Tetrahedron Lett. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Copper-mediated nucleophilic radiobromination of aryl boron precursors: Convenient preparation of a radiobrominated PARP-1 inhibitor
Tetrahedron Letters ( IF 1.8 ) Pub Date : 2018-04-11 , DOI: 10.1016/j.tetlet.2018.04.024
Dong Zhou , Wenhua Chu , Thomas Voller , John A. Katzenellenbogen

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.



中文翻译:

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

芳基硼前体与放射性溴离子的铜介导的亲核放射性溴化是一种有效且稳定的新型放射性标记方法。使用各种溶剂,温度和催化剂观察到高放射化学转化率(RCC)。该反应也是清洁的,并且对于纯化以获得高化学和放射化学纯度是可行的。该方法为制备包括溴标记的PARP-1抑制剂在内的放射性溴药物提供了非常有用的途径,它是对铜介导的放射性标记过程家族的宝贵补充。

更新日期:2018-04-11
down
wechat
bug