3508-24-5

Upstream product

• 71-43-2 benzene 
• 98-80-6 phenylboronic acid 
• 79-21-0 peracetic acid 
• 1626-00-2 phenyltrimethylgermane 
• 20461-54-5 [131I]iodide 

Relevant academic research and scientific papers

Radioactive iodine labeling method

The invention discloses a radioactive iodine labeling method. Ar-B(OH)2 is allowed to react with NaI in a reaction solvent in the presence of a copper coordination compound so as to obtain Ar-I, so radioactive iodine labeling is realized. The method

A Highly Efficient Copper-Mediated Radioiodination Approach Using Aryl Boronic Acids

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.

Direct n.c.a. electrophilic radioiodination of deactivated arenes with N-chlorosuccinimide

An efficient method for the direct electrophilic no-carrier-added (n.c.a.) radioiodination of deactivated arenes has been developed using N-chlorosuccinimide (NCS)/radioiodide in trifluoromethanesulfonic acid (triflic acid). Optimization of the one pot labelling procedure using chlorobenzene as a model substrate resulted in a radiochemical yield of 75% within 15 min at room temperature. Drying of the aqueous radioiodide solution prior to radiolabelling was not required. Radioiodination of weakly activated and deactivated monosubstituted benzene derivatives gave rise to radiochemical yields of about 80% with an electrophilic substitution pattern. Strongly deactivated aromatic compounds were radioiodinated with high radiochemical yields of about 70% exclusively in their meta-position using a reaction temperature of 75°C and a reaction time of 1 h. With regard to the reaction mechanism, in situ formed radioiodo(I) trifluoromethanesulfonate (triflyl [131I]hypoiodite) is discussed as electrophilic reagent.

No-carrier-added Radiobromination and Radioiodination of Aromatic Rings using In Situ Generated Peracetic Acid

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.