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Citation: FENG Zhi-Ming, YAN Zheng-Li, LI Xu-Hong, LI Feng, LEI Chun-Hua. Synthesis,Stability and Relaxivity of N-Alkyl-DO3A and Their Gd(Ⅲ) Chelates[J]. Chinese Journal of Applied Chemistry, ;2008, 25(8): 922-925. shu

Synthesis,Stability and Relaxivity of N-Alkyl-DO3A and Their Gd(Ⅲ) Chelates

1.
a College of Chemistry and Chemical Engineering, Hunan Normal University, Changsha 410081;
2.
b The Third Xiangya Hospital, Centralsouth University, Changsha

Corresponding author: FENG Zhi-Ming,
Received Date: 12 August 2007
Available Online: 25 October 2007
Fund Project: 湖南省教育厅资助科研项目(04C346) (04C346)

Synthesis of DO3A derivatives(H3L) modified by linear alkyl groups, N-hexyl-DO3A(2), N-decyl-DO3A(3), N-hexadecyl-DO3A(4), and their Gd(Ⅲ) chelates(GdL) is described. The protonation constants of compounds 2, 3 and 4, the stability constants and the water proton relaxivity of GdL were determined. The first protonation constants(lg K₁^H) of compounds 2, 3 and 4 were respectively 10.72, 10.68 and 10.52, the stability constants of the corresponing GdL chelates were respectively 20.50, 19.60 and 19.25, and the water proton relaxivitives(r₁) of the corresponding GdL chelates were respectively 4.88, 4.96 and 5.12 L/(mmol·S). The results obtained showed that the basicities of the ligands were all slightly altered, but the ligands still maintained strong chelating property and the water proton relaxivity of the parent DO3A after the introduction of a linear alkyl group at the cyclen backbone of DO3A.
- Gd(Ⅲ) chelate,
- DO3A derivative,
- stability,
- relaxivity
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