Preparation of an Amino Acid Based DTPA as a BFCA for Radioimmunotherapy

Bulletin of the Korean chemical society

Young-Don Hong¹  Kang-hyuk Choi¹  Sun-Ju Choi¹  Mi-Sun Pyun¹ 

关键词: DTPA derivative;    Amino acid;    166Ho-DTPA;    BFCA;    Radioimmunotherapy;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

For the purpose of developing more effective chelating agents, we have synthesized a diethylene triamine pentaacetic acid(DTPA) analogue by using an amino acid. S-(N-Boc-aminophenyl)-Cys(t-Bu₄-DTPA) methylester was prepared in 6 steps with total yield of 47.9%. For the sake of introducing a biomolecule to the DTPA derivative, a selective hydrolysis was performed with 3 M HCl/Ethylacetate = 1 : 3 (25 ∑C, 30 min, vigorous stirring). ¹⁶⁶Ho-Cys-DTPA and ¹⁶⁶Ho-Biotin-Cys-DTPA were prepared by mixing ¹⁶⁶Ho with DTPA derivatives at room temp in a HCl solution (pH = 5) and the radiochemical stabilities (> 99%) were maintained for over 6 hrs in vitro.

【 授权许可】

Unknown