Synthesis of DOTA-OIA and Physicochemical Characterization of Its Gd(III) Complex

• Main Authors: Iok-Sun Lei, 李毓璇
• Other Authors: Chai-Lin Hsu
• Format: Others
• Language: zh-TW
• Published: 2010
• Online Access: http://ndltd.ncl.edu.tw/handle/03589625003821062214

碩士 === 高雄醫學大學 === 醫藥暨應用化學研究所 === 98 === This research is focusing on developing the Gd ligands which have potential to targeting contrast agent. The carboxylic acid terminal of 5-(1-bromoacatamido)-2,3-dihydro-1-oxo-1H-indene-2-acetic acid can be modified with appropriate peptide or other target specific residue to develop target specific MRI contrast agent for potential application in tumor imaging. This research is to develop a ligand which has the character of optimal lipophilicity. The calculated value obtained for [Gd(DOTA-OIA)] (miLogP = -4.147) is similar to that of MS-325 (-4.575) which is clinically used blood pool MRI contrast agent. Together with the help of 1H-NMR、and the identification of LC-MS. I have successfully synthesized 5-(1-bromoacatamido) -2,3- dihydro-1- oxo-1H-indene-2-acetic acid. With the result of identification of LC-MS, its molecule weight is 327.93 which meets the expectation value. The synthesis of [Gd(DOTA-OIA)] is still in progress and expected to complete soon. The synthesis of [Gd(DOTA-OIA)] will be completed and get the spectral of last step. By using 20MHz relaxometor to measure the relaxivity.