Rapid and Mild Syntheses of Radioiodine-Labeled Radiopharmaceuticals

Radioiodine-labeled pharmaceuticals have been used extensively in diagnostic nuclear medicine. We have developed a rapid and mild method for incorporating radioiodine into functionally substituted molecules. The new process involves the reaction of the radioiodide ion with organoboranes in the presence of gentle oxidizing reagents. The radioiodide is utilized nearly quantitatively in a matter of seconds. The radiochemical yields are excellent, and parallel those obtained when iodine monochloride is reacted with organoboranes.