Macrocyclic complexes of yttrium, the lanthanides and the actini

Organic compounds -- part of the class 532-570 series – Organic compounds – Rare earth containing


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534 10, 5303915, 530402, 530409, 540465, 540474, A61K 4900, A61K 39395, C07F 500, C07D22100




Functionalized water soluble macrocyclic complexes of lanthanide, actinide and yttrium ions were obtained by metal templated, Schiff-base, cyclic condensation of: (1) a functionalized 1,2-diaminoethane and a dicarbonyl compound selected from the group consisting of 2,6-dicarbonylpyridine, 2,6-diformylpyridine, 2,5-dicarbonylfuran, 2,5-diformylfuran, 2,5-dicarbonylthiophene and 2,5-diformylthiophene; or (2) 1,2-diaminoethane and a ring-substituted heterocyclic dicarbonyl compound selected from a group consisting of substituted 2,6-dicarbonylpyridine, substituted 2,6-diformylpyridine, substituted 2,5-dicarbonylfuran, substituted 2,5-diformylfuran; substituted 2,5-dicarbonyl thiophene, and substituted 2,5-diformylthiophene. Coordination complexes thus formed are kinetically stable in dilute aqueous solution. They are further reacted, or coupled, through a substituent on the 1,2-diaminoethane or on the pyridine, furan, or thiophene moieties, to one of the following: proteinaceous materials, polysaccharides, other biologically compatible macromolecules or bridging molecules which, can be further reacted or coupled to the above mentioned substrates. These macrocyclic complexes are suitable in the preparation of reporter molecules and for magnetic resonance, radiation imaging and radiation therapy.

patent: 4454106 (1984-06-01), Gansow et al.
patent: 4678667 (1987-07-01), Meares et al.
patent: 5087696 (1992-02-01), Parker et al.
Derwent Abstract 89-062473/09, Hoescht AG, EP 304, 780 A, Aug. 1987.
Desreux et al., Nucl. Med. Biol., vol. 15, No. 1 (1988) pp. 9-15.
Abid et al., Inorganica Chim. Acta, vol. 95 (1984) pp. 119-125.


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