N-(1-p-nitrobenzaldhydephenyl)-2-(2-iodophenyl)-4-(4-nitrobenzilidene)-imidazolin-5-onewas labeled with radioactive iodine-125.via nucleophilic substitution reaction, the isotopic exchange labeling process was carried out in dry state at 330oC for 20 min. The radiochemical yield was determined by using electrophoresis and the yield is equal to 93%.Ammonium sulphate was used as catalyst to facilitate the exchange reaction in melt state. Maximum heated with iodine-125 at 330oC for 20 min in a reaction mixture with pH between 6 and 8. The results referred to the importance of use NaOH in a molarity of less than 0.02M to prevent the decomposition of the produced tracer due to the change in pH of the reaction mixture. The biodistrubution pattern of the labeled compound was examined in normal as well as in tumor bearing mice and the data show high clearance from the blood as the activity remind in the blood 11.2% at 4 hours post injection. The labeled compound was extracted via liver as the accumulated activity in the liver and intestine were 14.4, 15.4% respectively at 4 hours post injection The biodistrubution of labeled compound in tumor bearing mice accumulation in ascites with high percentage equal to 55.3 % at 24 hours post injection. This demonstrate the ability of this tracer concentrate in tumor site which primate its possible application as therapeutic agent.

How to cite this article: Labib AA, Challan MB. Synthesis, Radioiodination and Biological distribution of 5-(5-(tributylstannyl) benzofuran-2-yl) pyridin-2-amine as an amyloid imaging agent. J Radiol Oncol.

This study describe the organic synthesis of 2-iodobenzamido (2-N-nitrobenzen-5, 6, 7, 8 tetrahydrobenzothieno [2, 3-d]) pyrimidine -4-(3H) one as an example for some pyrimidine derivative used a new series of as potential cancer chemotherapeutic agents. The precursor derivative is α-(2-iodobenzamido)-β -(4-nitrophenyl)-N-[3-ethoxy-carbonyl-4, 5, 6, 7-tetrahydrobenzothiophen-2-l] acrylic acid amide which react with hydrazine hydrate. The purification process was done via crystallization using solvent ethanol. The overall yield 78% the structure of the synthesized compound was confirmed by correct analytical and spectral data .Also, The synthesized compound was labeled with radioactive iodine -125 via nucleophilic substitution reaction ,in the presence cuprous chloride, the labeling process was carried out at 95oC for 60 min. the radiochemical yield was determined by using thin layer chromatography and the yield is equal to 80%.Preliminary in-vivo study was examined in normal mice were performed after intravenous injection through the tail vein and the data show the labeling compound was cleared quickly from most body organs. The radioiodinated compound showed high brain uptake .The results in this study suggest that radioiodinated pyrimidine derivative may be useful as cancer chemotherapeutic agents.