A new efficient method for the preparation of 99mTc-radiopharmaceuticals containing the TcN multiple bond

International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes Pub Date : 1992-11-01 DOI:10.1016/0883-2889(92)90004-X

Roberto Pasqualini , Veronique Comazzi , Emmanuel Bellande , Adriano Duatti , Andrea Marchi

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引用次数: 63

Abstract

An improved method for the preparation of ^99mTc-radiopharmaceuticals containing the TcN multiple bond, in sterile and apyrogen conditions, is described. This method is based on the reaction of [^99mTc]pertechnetate with ligands derived from S-methyl dithiocarbazate [H₂NN(R)C(S)SCH₃ [R = H, CH₃], in the presence of HCl and tertiary phosphines. It was found that these derivatives can behave both as sources of nitride nitrogen ions (N³⁻) and as coordinating ligands. The reaction leads to the formation of intermediate technetium-nitrido complexes in high yield. These intermediate species can be used as suitable prereduced substrates for the preparation of technetium-nitrido radiopharmaceuticals through simple substitution reactions with appropriate exchanging ligands.

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一种制备含TcN多键的99mtc -放射性药物的新方法

本文描述了一种在无菌和无氧条件下制备含有TcN多键的99mtc -放射性药物的改进方法。该方法是基于[99mTc]高技术酸盐与S-甲基二硫代氨基甲酸盐[H2NN(R)C(S)SCH3 [R = H, CH3]衍生的配体在HCl和叔膦存在下的反应。发现这些衍生物既可以作为氮化氮离子(N3−)的来源，也可以作为配位体。该反应生成了高收率的中间技术氮络合物。这些中间物质可以作为合适的预还原底物，通过与适当的交换配体进行简单的取代反应，制备锝-硝基放射性药物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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International Journal of Radiation Applications and Instrumentation. Part A. Applied Radiation and Isotopes

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