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

Research output: Contribution to journalArticle

5 Scopus citations

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.

Original languageEnglish
Pages (from-to)1963-1967
Number of pages5
JournalTetrahedron Letters
Volume59
Issue number20
DOIs
StatePublished - May 16 2018

Keywords

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

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