Organic Synthesis and Technetium-99m Labeling of Some Amino-Phenol Ligands

We reported the synthesis and labeling of one tetradentate and two pentadentate amino-phenol ligands with technetium-99m by the direct pertechnetate addition and by ligand exchange methods. Labeling by direct pertechnetate addition was attended by adding pertechnetate eluate to the ethanolic solution of the amino-phenol ligands at pH 9. Stannous chloride dihydrate was used as reducing agent. Exchange studies were carried out via the use of the following 99mTc-chelates: 99mTc-DTPA, 99mTc-gluconate, 99mTc-tartrate and 99mTc-citrate complexes. Ligand exchange method was achieved by incubation the ligand solutions with 99mTc-co-ligands complexes in 0.05M bicarbonate buffer pH 9. At this pH value the 99mTc-co-ligands dissociated and the more stable new 99mTc-ligands were formed with high radiochemical yield ≥95%. The radiochemical yield of 99mTc-labeled amino-phenol ligands were estimated by solvent extraction, electrophoresis and HPLC methods. The produced technetium-99m amino-phenol complexes were neutral, lipophilic and stable during the period of 24 hours.