摘要
Technetium-99m-labeled-5-{2-sulfanylethyl-[2-(2-sulfanylethylamino)acetyl]amino}-methyl-2′-deoxy- uridine (99mTc-ANMdU) was reported. The precursor ANMdU was synthesized by six-step reactions and all intermediates were verified with MS and 1HNMR. Using SnCl2 as reducing agent, a labeling reaction was carried out at 100°C for 30 min. The radiochemical purity of the 99mTc-ANMdU was 96.68%. Partition coefficients were 0.92 and 0.70 at pH 7.0 and 7.4 of the phosphate buffer saline, respectively. Biodistribution of 99mTc-ANMdU in normal mice showed that the initial uptake of 99mTc-ANMdU in vivo and the clearance was rapid.
Technetium-^99m-labeled-5- {2-sulfanylethyl- [2-（2-sulfanylethylamino）acetyl]amino }-methyl-2＇-deoxy- uridine （^99mTc-ANMdU） was reported. The precursor ANMdU was synthesized by six-step reactions and all intermediates were verified with MS and 1HNMR. Using SnCl2 as reducing agent, a labeling reaction was carried out at 100℃ for 30 min. The radiochemical purity of the ^99mTc-ANMdU was 96.68%. Partition coefficients were 0.92 and 0.70 at pH 7.0 and 7.4 of the phosphate buffer saline, respectively. Biodistribution of ^99mTc-ANMdU in normal mice showed that the initial uptake of ^99mTc-ANMdU in vivo and the clearance was rapid.
基金
Supported by National Natural Science Foundation of China (20573048 and 20676051)
Natural Science Foundation of Jiangsu Province (BK2008111, BK2008112)
Department of Health of Jiangsu Province (H200624)
