SYNTHESIS AND RADIOLABELING OF A BIOTIN-CHX-B CHELATE FOR BI-213

The synthesis and radiolabeling of a biotin derivative which contains a chelating group (CHX-B) for binding the alpha-emitting radionuclide, Bi-213, is described. The biotin-CHX-B derivative was readily prepare d in high yield through a convergent synthesis that coupled N-methylgl ycylbiotinamide with anilino-CHX-B. Bismuth-213 labeling of the biotin -CHX-B molecule was facile at room temperature, resulting in >95 % rad iochemical yield within 10 min reaction time.