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 I-123-, I-125-, I-131-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).