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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 27, Number 8
BKCSDE 27(8)
August 20, 2006 

Preparation of an Amino Acid Based DTPA as a BFCA for Radioimmunotherapy
Kang-hyuk Choi, Young-Don Hong, Mi-Sun Pyun, Sun-Ju Choi*
DTPA derivative, Amino acid, 166Ho-DTPA, BFCA, Radioimmunotherapy
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.
1194 - 1198
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