The purpose of this article is to study the synthesis and radioiodination of the fullerene derivative con- taining active antitumor groups. The fullerene pyrrolidine benzoyl nitrogen mustard was synthesized by 1

3 di- pole[3+2] cycloaddition reaction with fullerene

N-methylglycine and N

N-bis(2-chloroethyl)-4-aminobenzaldehyde. Its chemical structure was characterized by the spectroscopic data. The synthesized compound

after connected with the stable iodine

was radiolabeled with iodine-125 through isotope exchanging. Dependences of radiolabeling yields on both reaction temperature and exchanging-time were examined. The results showed that the radiolabeling yield of fullerene pyrrolidine benzoyl nitrogen mustard was as high as 94 % after heating for 2 hours at 130℃.