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首页> 外文期刊>Inorganic Chemistry: A Research Journal that Includes Bioinorganic, Catalytic, Organometallic, Solid-State, and Synthetic Chemistry and Reaction Dynamics >(S)-(2-(2'-Pyridyl)ethyl)cysteamine and(S)-(2-(2'-Pyridyl)ethyl)-D,L-homocysteine as Ligands for the 'feo[M(CO)_3]~+'(M=Re,~(99m)Tc)Core
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(S)-(2-(2'-Pyridyl)ethyl)cysteamine and(S)-(2-(2'-Pyridyl)ethyl)-D,L-homocysteine as Ligands for the 'feo[M(CO)_3]~+'(M=Re,~(99m)Tc)Core

机译:(S)-(2-(2'-吡啶基)乙基)半胱胺和(S)-(2-(2'-吡啶基)乙基)-D,L-高半胱氨酸作为“ fe [M(CO)_3”的配体]〜+“(M = Re,〜(99m)Tc)核心

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摘要

The reaction of fac-[NEt_4]_2[Re(CO)_3Br_3] with(S)-(2-(2'-pyridyl)ethyl)-cysteamine,LI,in methanol leads to the formation of the cationic fac-[Re(CO)_3(NSN)][Br] complex,1,with coordination of the nitrogen of the pyridine,the sulfur of the thioether,and the nitrogen of the primary amine.When fac-[NEt_4]_2[Re(CO)_3Br_3] reacts with the homocysteine derivative(S)-(2-(2'-pyridyl)ethyl)-D,L-homocysteine,L_2,the neutral fac-Re(CO)_3(NSO)complex,2,is produced with coordination of the nitrogen of the primary amine,the sulfur of the thioether,and the oxygen of the carboxylate group,while the pyridine ring remains uncoordinated.The analogous technetium-99m complexes,1' and 2',were also prepared quantitatively by the reaction of L_1 and L_2 with the fac-[~(99m)Tc(CO)_3(H_2O)_3]~+ precursor at 70 deg C in water.Given that both(S)-(2-(2'-pyridyl)ethyl)cysteamine and homocysteine can be easily N-or S-derivatized by a bioactive molecule of interest,both the NSN or NSO ligand systems could be used to develop target-specific radiopharmaceuticals for diagnosis and therapy.
机译:fac- [NEt_4] _2 [Re(CO)_3Br_3]与(S)-(2-(2'-吡啶基)乙基)-半胱胺在甲醇中的反应导致阳离子fac- [Re (CO)_3(NSN)] [Br]配合物1,与吡啶的氮,硫醚的硫和伯胺的氮配位。当fac- [NEt_4] _2 [Re(CO) _3Br_3]与高半胱氨酸衍生物(S)-(2-(2'-吡啶基)乙基)-D,L-高半胱氨酸,L_2反应,生成中性的fac-Re(CO)_3(NSO)络合物2,伯胺的氮,硫醚的硫和羧酸根的氧配位,而吡啶环仍不配位。还通过反应定量制备了类似--99m的配合物1'和2'。于70℃下在水中于水中用fac- [〜(99m)Tc(CO)_3(H_2O)_3] +前体合成L_1和L_2。给出(S)-(2-(2'-吡啶基)乙基半胱胺和高半胱氨酸可以很容易地被感兴趣的生物活性分子进行N-或S-衍生,无论是NSN还是NSO配体系统都可以使用o开发用于诊断和治疗的靶标特异性放射性药物。

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