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 [H 2NN(R)C(S)SCH 3 [R = H, CH 3], in the presence of HCl and tertiary phosphines. It was found that these derivatives can behave both as sources of nitride nitrogen ions (N 3−) 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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