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RADIOACTIVE TRANSMISSION METAL-IMIDO-HETERODIPHOSPHINK COMPLEMENTS; THEIR MANUFACTURE AND RADIOPHARMAZEUTIC SUMMARIES
RADIOACTIVE TRANSMISSION METAL-IMIDO-HETERODIPHOSPHINK COMPLEMENTS; THEIR MANUFACTURE AND RADIOPHARMAZEUTIC SUMMARIES
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机译:放射性金属-亚胺基-异硫氰酸盐的放射性补体;他们的制造和放射性药物概述
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摘要
The present invention provides radioactive metal heterocomplexes of formula (I): Ä(Me=N-R)L1L2Ü+Z- wherein Me, R, L1 L2 and Z- have the meanings indicated in the description. The complexes include a trivalent radioactive metal-imido group, typically a technetium- or rhenium-imido group, strongly stabilized by the presence of an ancillary tridentate hetero-diphosphine ligand L1, which allows the formation of substitution-inert Ä(Me=N-R)L1Ü moieties. Such moieties are fixed in an intermediate Ä(Me=N-R)Y2L1)Ü+ compound which contains two labile, cis-positioned, Y ligands, where Y is preferably an halide group. The latter are easily replaced by a bidentate ligand L2 to give the final Ä(Me=N-R)L1L2Ü+Z- heterocomplexes. The complexes of the invention are useful for the preparation of radiopharmaceuticals: in fact, a bioactive fragment which confers biological target-seeking properties can be introduced either on the L2 framework or the imido R group.
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机译:本发明提供式(I)的放射性金属杂配合物:Ä(Me = NR)L 1 L 2Ü+ Z--其中Me,R,L 1 L 2和Z <->具有描述中指示的含义。该配合物包括三价放射性金属亚氨基,通常为tech或im亚氨基,可通过存在辅助三齿杂二膦配体L 1来稳定,从而形成惰性取代基(Me = NR)L 1Ü部分。这样的部分被固定在中间的(Me = N-R)Y 2 L 1)Ü+化合物中,该化合物包含两个不稳定的,顺式定位的Y配体,其中Y优选为卤基。后者容易被二齿配体L 2取代,得到最终的Ä(Me = N-R)L 1 L 2 L +Ü+ Z-杂配合物。本发明的复合物可用于制备放射性药物:实际上,赋予生物学靶标寻找特性的生物活性片段可被引入到L 2构架或亚氨基R基团上。
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