Copper-Mediated Nucleophilic Radiobromination of Aryl Boron Precursors: Convenient Preparation of a Radiobrominated PARP-1 Inhibitor.

Dong Zhou,Wenhua Chu,Thomas Voller,John A Katzenellenbogen

Tetrahedron Letters（2018）

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摘要

•Copper-mediated nucleophilic radiobromination of aryl boron precursors.•Broad scope of aryl boron precursors.•Efficient and robust radiolabeling reactions.•High yield and feasible purification.•Used for the facile synthesis of a radiobrominated PARP-1 inhibitor.

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关键词

Labeling method,Nucleophilic radiobromination,Boron reagents,Bromine-76,Bromine-77,Auger electron radiation,PET imaging

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