81823-95-2Relevant academic research and scientific papers
A Highly Efficient Copper-Mediated Radioiodination Approach Using Aryl Boronic Acids
Zhang, Pu,Zhuang, Rongqiang,Guo, Zhide,Su, Xinhui,Chen, Xiaoyuan,Zhang, Xianzhong
, p. 16783 - 16786 (2016)
A convenient and quantitative radioiodination method by copper-mediated cross-coupling of aryl boronic acids was developed. The mild labeling conditions, ready availability of the boronic acid substrate, simple operation, broad functional group tolerance and excellent radiochemical yield (RCY) make this a practical strategy for radioiodine labeling without further purification.
Regiospecific No-Carrier-Added Radiobromination and Radioiodination of Arylmethyl Group IVb Organometallics
Moerlein, Stephen M.,Coenen, Heinz H.
, p. 1941 - 1948 (2007/10/02)
A series of para-substituted aryltrimethyl-silicon, -germanium, and -tin compounds were treated at room temperature with no-carrier-added (n.c.a.) 77Br and 131I to compare their utility as substrates for regiospecific aromatic halogenation.Dichloramine-T was used as an in situ oxidant in acidic, polar, or non-polar reaction solvents.N.c.a. aromatic halodemetallation was regiospecific for all substrates, radiochemical yields were generally higher for 131I than 77Br, and halogenation yields increased as Si Ge Sn.Arguments are presented for a substitution mechanism involving a ?-complex intermediate with bond formation as the yield-determinig step.Although high yields were obtained for the n.c.a. aromatic halogenodestannylations irrespective of aromatic substituent or solvent, significant chlorination occured as a side-reaction.N.c.a. aromatic halogenodegermylation produced high radiochemical yields with insignificant chlorination, but the radiohalogenation yields were sensitive to ring deactivation and solvent effects.N.c.a. aromatic halogenodesilylation gave high yields only in activated aromatic systems.The relative benefits of each demetallation reaction for regiospecific n.c.a. radiolabelling or preparative halogenation of aromatic rings are outlined.
