Radiolabeling kit/generator for 5-radiohalogenated uridines

A rapid, simple and inexpensive synthesis of 5-radiohalogenated-2′-deoxyuridine from 5-trimethylstannyl-2′-deoxyuridine is described. The total reaction and purification time including thin layer chromatography (tlc) for quality control is less than 30 min. This method produces excellent yields (>95%) of 123I-, 125I-, 131I-UdR. The radiochemical purity of all tested preparations (>20) was determined to be greater than 99%. This new method is the basis of a radiolabeling kit/generator for preparation of radiohalogenated nucleosides. 2′-Deoxyuridine (UdR) halogenated with a stable isotope of bromine was also synthesized indicating that the method can be applied to the preparation of 5-radiobromo-2′-deoxyuridine (BUdR).