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水溶液中新核心[99Tc(CO)2(NO)]2+和[99Tcm (CO)2(NO)-L] (L=DTPA, EDTA, EHIDA)的制备

刘晶莹, 杨洋, 朱霖

刘晶莹, 杨洋, 朱霖. 水溶液中新核心[99Tc(CO)2(NO)]2+和[99Tcm (CO)2(NO)-L] (L=DTPA, EDTA, EHIDA)的制备[J]. 核化学与放射化学, 2009, 31(2): 90-97.
引用本文: 刘晶莹, 杨洋, 朱霖. 水溶液中新核心[99Tc(CO)2(NO)]2+和[99Tcm (CO)2(NO)-L] (L=DTPA, EDTA, EHIDA)的制备[J]. 核化学与放射化学, 2009, 31(2): 90-97.
LIU Jing-ying, YANG Yang, ZHU Lin. Preparation of New Core [99Tcm (CO)2(NO)]2+ and Its Derivatives [99Tcm (CO)2(NO)L] (L=DTPA, EDTA, EHIDA) in Aqueous Solution[J]. Journal of Nuclear and Radiochemistry, 2009, 31(2): 90-97.
Citation: LIU Jing-ying, YANG Yang, ZHU Lin. Preparation of New Core [99Tcm (CO)2(NO)]2+ and Its Derivatives [99Tcm (CO)2(NO)L] (L=DTPA, EDTA, EHIDA) in Aqueous Solution[J]. Journal of Nuclear and Radiochemistry, 2009, 31(2): 90-97.

水溶液中新核心[99Tc(CO)2(NO)]2+和[99Tcm (CO)2(NO)-L] (L=DTPA, EDTA, EHIDA)的制备

Preparation of New Core [99Tcm (CO)2(NO)]2+ and Its Derivatives [99Tcm (CO)2(NO)L] (L=DTPA, EDTA, EHIDA) in Aqueous Solution

  • 摘要: 研究了水溶液中制备[99Tcm (CO)2(NO)-L](L=DTPA, EDTA, EHIDA)配合物的2种方法:(1) 由前体[99Tcm (CO)3-L]制备[99Tcm (CO)2(NO)-L]; (2) 由[99Tcm (CO)2(NO)(H2O)3]2+中间体制备[99Tcm (CO)2(NO)-L];并确定了最佳标记条件。TLC和HPLC结果表明,2种方法得到的配合物放化产率均在90%以上。初步建立了1套在水溶液中简单、高效制备新的[99Tcm (CO)2(NO)]2+类配合物的方法。[NO]+基团取代原三羰基锝配合物得到的[99Tcm (CO)2(NO)-L]配合物具有良好的体外稳定性,取代后的配合物脂溶性和电荷性质都发生了改变,为99Tcm放射性药物的研制开辟了新思路。
    Abstract: In order to develop a new method for the preparation of the [99Tcm (CO)2(NO)-L] (L=DTPA, EDTA, EHIDA) complexes in aqueous solution, two different procedures were developed: one is formation of the metal-tricarbonyl-ligand complex and subsequent nitrosylation; another is nitrosylation of the metal-tricarbonyl precursor followed by reaction with the ligand. The optimal labeling conditions were studied. Results of TLC and HPLC indicate that the radiochemical yields derived from the two methods list above are all more than 90%. It’s an easier new way to prepare [99Tcm (CO)2(NO)-L] complexes in aqueous solution with high efficiency. The newly developed [99Tcm (CO)2(NO)-L] complexes are stable at room temperature during 1 half-life of the isotope. At the same time, the lipophility and net charge of [99Tcm (CO)2(NO)-L]complexes are also changed comparing with that of corresponding [99Tcm(CO)3]+core complexes. It opens a new field for designing radiopharmaceuticals. 
  • [1] Roger A, Roger S, Andre E, et al. A Novel Organometallic Aqua Complex of Technetium for the Labeling of Biomolecules: Synthesis of [99Tcm(OH2)3(CO)3+ From [99TcmO4]- in Aqueous Solution and Its Reaction With a Bifunctional Ligand[J]. J Am Chem Soci, 1998, 120: 7 987-7 988.
    [2] Alberto R, Schibli R, Waibel R, et al. Basic Aqueous Chemistry of [M(OH2)3(CO)3]+ (M=Re, Tc) Directed Towards Radiopharmaceutical Application[J]. Coord Chem Rev, 1999, 190-192: 901-919.
    [3] 张小波,朱霖,赵学颖,等.[99Tcm (CO)3(H2O)3]+ 标记的新双功能连接剂的研究[J].核化学与放射化学,2004, 26(1): 11-17.
    [4] Chu T W, Zhang Y, Liu X Q, et al. Synthesis and Biodistribution of 99Tcm-Carbonyltechnetium-Labeled Fatty Acids[J]. Appl Radia Isot, 2004, 60(6): 845--850.
    [5] Alves S, Paulo A, Correia J D G, et al. Pyrazolyl Derivatives as Bifunctional Chelators for Labeling Tumor-Seeking Peptides With the fac-[M(CO)3]+ Moiety (M=99Tcm, Re): Synthesis, Characterization, and Biological Behavior[J]. Bioconjugate Chem, 2005, 16: 438-449.
    [6] Lazarova N, Babich J, Valliant J, et al. Thiol--and Thioether-Based Bifunctional Chelates for the {M(CO)3}+Core (M =Tc, Re)[J]. Inorg Chem, 2005, 44: 6 763-6 770.
    [7] Rattat D, Verbruggen A, Schmalle H, et al. [M(CO)2(NO)]2+, a New Core in Bioorganometallic Chemistry: Model Complexes of [Re(CO)2(NO)]2+and [99Tcm(CO)2(NO)]2+[J]. Tetrahedron Lett, 2004, 45: 4 089-4 092.
    [8] Rattat D, Terwinghe C, Verbruggen A. Comparison of “Classic” 99Tcm–DTPA, 99Tcm(CO)3-DTPA and 99Tcm(CO)2(NO)–DTPA[J]. Tetrahedron, 2005, 61: 9 563-9 568.
    [9] Yang Y, Zhang J X, Wang J J, et al. Two Novel Procedures of Preparation for [99Tcm(CO)2(NO)]2+Labeled by EHIDA and Its Biodistribution[J]. J Radioanal Nucl Chem, 2007, 273: 31-36.
    [10] Rattat D, Verbruggen A, Berke H, et al. Exploring the Nitrosyl-Approach: “Re(CO)2(NO)”and “Tc(CO)2(NO)”-Complexes Provide New Pathways for Bioorganometallic Chemistry[J]. J Organomet Chem, 2004, 689: 4 833-4 836.
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出版历程
  • 收稿日期:  2007-10-17
  • 修回日期:  2008-05-21
  • 刊出日期:  2009-05-19

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