84600-74-8Relevant articles and documents
Copper-mediated nucleophilic radiobromination of aryl boron precursors: Convenient preparation of a radiobrominated PARP-1 inhibitor
Zhou, Dong,Chu, Wenhua,Voller, Thomas,Katzenellenbogen, John A.
supporting information, p. 1963 - 1967 (2018/04/23)
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.
No-carrier-added Radiobromination and Radioiodination of Aromatic Rings using In Situ Generated Peracetic Acid
Moerlein, Stephen M.,Beyer, Werner,Stoecklin, Gerhard
, p. 779 - 786 (2007/10/02)
Peracetic acid generated in situ from aqueous hydrogen peroxide and glacial acetic acid was examined as an oxidizing agent for electrophilic aromatic bromination and iodination without chlorinated side products.No-carrier-added (n.c.a.) 77Br and 131I were used with simple organic aromatic compounds or aryltrimethyl-tin, -germanium, and -silicon organometallic compounds to identify reaction parameters which influence this electrophilic halogenation method.N.c.a. aromatic halogenodeprotonation using peracetic acid was relatively slow and resulted in high labelling yields only with aromatic rings that were activated toward electrophilic substitution.By contrast, high radiochemical yields were rapidly obtained via iododestannylation of aromatic rings regardless of their degree of electronic activation.Useful labelling yields were also achieved using bromodestannylation reactions with aromatic rings deactivated toward electrophiles, but optimum yields with activated systems required the use of germylated arenes as substrates.The practical aspects of aromatic halogenodemetallation and halogenodeprotonation as n.c.a. electrophilic halogenation techniques with in situ generated peracetic acid are outlined.
