摘要
A novel zoledronic acid derivative,1-hydroxy-2-(2-butyl-1H-imidazole-1-yl)-ethylidene-l,l- diphosphonic acid(BIDP),was synthesized and labeled with ^(99)Tc^m.The detailed kinetic study on the labeling reaction between BIDP and ^(99)Tc^m was carried out.The results indicated that the reaction rate constants k were 0.0258,0.0268, 0.0305,0.0323,0.0351 and 0.0384 min^(-1)at 0℃,5℃,10℃,15℃,20℃and 25℃,respectively.From the Arrhenius equation k=A·e^(-E_Δ/(RT)),the activation energy E_a of the labeling reaction was calculated to be 10.45 kJ/mol.And the correlation between k and temperature(T)was also deduced as In k=-1258.8×(l/T)+0.9531.In addition,it was found that in order to get a high radiolabeling yield(RLY)(>90%),the reaction temperature must be up to 12℃.
A novel zoledronic acid derivative, l-hydroxy-2-(2-butyl- 1H-imidazole- !-yl)-ethylidene- 1,1- diphosphonic acid (BIDP), was synthesized and labeled with 99TCm. The detailed kinetic study on the labeling reaction between BIDP and 99Tcm was carried out, The results indicated that the reaction rate constants k were 0.0258, 0.0268, 0.0305, 0.0323, 0.0351 and 0.0384 rain-~ at 0~C, 5~C, 10~C, 15~C, 20~C and 25~C, respectively. From the Arrhenius equation k=-A.e e~/(eT~, the activation energy Ea of the labeling reaction was calculated to be 10.45 k J/tool. And the correlation between k and temperature (T) was also deduced as In k---1258.8x(1/7)+0.9531. In addition, it was found that in order to ~,et a high radiolabelinu vield (RI.Y~ (〉 q0%~ the, ronetinn tomnornt,,ro t h tc~ I '~o~~
基金
Supported by National Natural Science Foundation of China(Nos.20801024 and 21001055)
Natural Science Foundation of J iangsu Province(No.BK2009077)
Science Foundation of Health Department of Jiangsu Province(No.H200963)