Several derivatives of cyclopentadienylcobalt complexes having a pendant amino-functionalised side chain (CpЈ) are described, the cyclopentadienyl ligands being (2-aminoethyl)cyclopentadienyl, (2-piperidinoethyl)cyclopentadienyl, 1-(2-piperidinoethyl)-2,3,4,5-tetraisopropylcyclopentadienyl and 2-picolylcyclopentadienyl. Chelation by the amino-functionalised side chain occurred when the Cp*-cobalt(I) dicarbonyl complexes 5, 6, 7 and 8 were oxidised by iodine, thereby forming the corresponding Cp*-cobalt(III) chelates 9, 10, 11 and 12, respectively, through the diiodocarbonyl intermediates 5Ј, 6Ј, 7Ј and 8Ј, respectively. The stabilities of the intermediates differ greatly due to the different amino functions in the pendant side chain. Structural studies of 9, 10 and 12 were carried out and the correlation of the I-Co-I
Three linear mercaptoacetyl tetrapeptides, MAG3-Leu-OH, MAG3-Phe-OH and MAG3-Tyr-OH, were synthesized via a liquid phase synthetic approach with high yields and high purities without using preparative HPLC technique. The obtained products could be radiolabeled easily with 99m Tc under a mild condition and showed high stability in vitro and in vivo conditions. The scintigrams of the tested rabbit after injection of the radiolabeled products via mainline showed a normal biodistribution, which is definitely different from that of 99m Tc-MAG3, indicating different routes of metabolization between these two radiochemicals.
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