No-carrier-added radiohalogenations utilizing organoboranes: The synthesis of iodine-123 labeled curcumin

Investigation on the reactivity of nucleophilic radiohalogens with arylboronic acids in water: access to an efficient single-step method for the radioiodination and astatination of antibodies

“…This hypothesis is supported by previous studies having reported on the radioiodination of aryltrifluoroborate or arylboronic acid precursor using electrophilic radioiodide, in the presence or absence of a catalyst. 34,35 We then probed the possibility to reduce the precursor concentration to a level acceptable for mAb radiolabelling. No drop in RCYs was observed when precursor concentration was decrease to 250 μM, a condition being chosen as it corresponds approximately, in terms of available arylboronic groups, to a solution of mAb concentrated at 6 mg mL −1 with a ratio of 6 arylboronic acids grafted per mAb.…”

“…This hypothesis is supported by previous studies having reported on the radioiodination of aryltrifluoroborate or arylboronic acid precursor using electrophilic radioiodide, in the presence or absence of a catalyst. 34,35 . We then probed the possibility to reduce the precursor concentration to a level acceptable for mAb radiolabelling.…”

Radioiodination of polymer‐supported organotrifluoroborates

“…Organoboron compounds are useful precursors for radiopharmaceutical preparations due to their ready availability and low toxicity. Over the years, we have developed several methods for incorporating short‐lived and long‐lived isotopes into useful molecules based on organoborane, organoboronic acid, and organotrifluoroborate intermediates 4, 5. We also evaluated the use of polymeric organoborane reagents a number of years ago 1.…”

Radiolabeling of Theranostic Nanosystems

“…Radioisotope production is globally concentrated on facilities with accelerators and reactors. Smaller medical cyclotrons capable for the production of short-lived positron emitters ( 11 C, 13 N, 15 O, 18 F, 89 Zr, 124 I) are available at academic institutions and hospitals to account for the heavy use of these isotopes in the clinic and the fact that some of them cannot be transported due to the short half-life (< 2 hours). Also 99 Mo/ 99m Tc and 68 Ge/ 68 Ga generators are nowadays nearly ubiquitous in research and hospital laboratories because of their long usable life time which allows the users to dispense the radioisotope on demand.…”

“…Boron derivatives also have low toxicity and boron compounds such as boronate esters and trifluoroborate salts are air stable crystalline solids making them ideal precursors for halodemetallation reactions. [15] The boronate esters and trifluoroborate salts can be regioselectively prepared using the Miyaura borylation reaction which is the coupling…”