SYNTHESIS OF NEW BIFUNCTIONAL CHELATING-AGENTS - NE-1,2-DIAMINE-N,N,N',N'-TETRAKISMETHANEPHOSPHONIC ACID (4-ICMP) AND ANE-1,2-DIAMINE-N,N,N',N'-TETRAKISETHANEPHOSPHONIC ACID (4-ICEP)

Immunotherapy with radiolabelled antibodies should allow fairly specif ic targeting of certain cancers, Although Sm-153 possesses favourable radiophysical characteristics for such therapy, a lack of radiolabelli ng stability in vivo limits its application, Yet the use of phosphonic semi-rigid bifunctional chelating agents (BCA) can improve its stabil ity, Syntheses of ne-1,2-diamine-N,N,N',N'-tetrakismethanephosphonic a cid (4-ICMP) and ane-1,2-diamine-N,N,N',N'-tetrakisethanephosphonic ac id (4-ICEP) are described in this paper, The complexing properties of these two compounds has been confirmed by labelling with Sm-153. A nov el synthetic approach involving the introduction of methanephosphonic functions has also been developed.