Closo-dodecarborate (2−) was proposed as a prosthetic group for direct labelling of proteins with 211At for radionuclide therapy. Astatination of closo-dodecarborate (2−) anion using Chloramine-T was studied, and the influence of pH, reaction time, amount of substrate and oxidant was determined. A maximum labelling yield of 55–75% was found in the pH range 7–8. A spontaneous astatination of closo-dodecarborate (2−) in the absence of Chloramine-T was also found, presumably due to generation of oxidising products from water radiolysis. Our results indicate that derivatives of closo-dodecarborate (2−) anion may be used as prosthetic groups for direct labelling of proteins.
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Orlova et al. (2000) studied this question.