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合成了用直链烷基修饰的DO3A衍生物(H3L):N-己基-DO3A(2)、N-癸基-DO3A(3)和N-十六烷基-DO3A(4)及其钆(Ⅲ)螯合物,测得化合物2、3和4的第1级质子化常数(lgK1H)分别为10.72、10.68和10.52;相应的钆(Ⅲ)螯合物的稳定常数(lgKGdL)分别为20.50、19.60和19.25;相应的钆(Ⅲ)螯合物的水质子弛豫率(R1)分别为4.88、4.96和5.12L/(mmol·S)。结果表明,在DO3A的1,4,7,10-四氮杂环十二烷骨架上引入直链烷基,其碱性略有改变,但仍保持DO3A母体的强螯合性能和水质子弛豫率。
DO3A derivatives (H3L) modified with linear alkyl groups were synthesized: N-hexyl-DO3A (2), N-decyl-DO3A (3) and N-hexadecyl-DO3A Ⅲ) chelates. The first order protonation constants (lgK1H) of compounds 2, 3 and 4 were found to be 10.72, 10.68 and 10.52, respectively. The stability constants (lgKGdL) of corresponding gadolinium chelates were 20.50 , 19.60 and 19.25 respectively. The water proton relaxation rate (R1) of the corresponding gadolinium (Ⅲ) chelates was 4.88, 4.96 and 5.12 L / (mmol · S), respectively. The results showed that the linear alkyl group was introduced into the 1,4,7,10-tetraazacyclododecane skeleton of DO3A and its basicity changed slightly, but the strong chelation performance of DO3A precursor and water proton relaxation Yu rate.