G.Ergun Efe, M. Pillai, E. O. Schlemper
1991
Citations
0
Influential Citations
17
Citations
Journal
Polyhedron
Abstract
The syntheses of a new, bifunctional ligand, 3-[N-(4-aminobenzyl)]amino-3- methyl-2-butanone oxime, ligand I , and a non-bifunctional analogue 3-benzylamino-3- methyl-2-butanone oxime, ligand II , the former for labelling proteins with 105 Rh complexes for internal radiotherapy applications are reported. The rhodium complex of ligand II was isolated and characterized by 1 H NMR, IR spectroscopy and X-ray crystallography. The crystal structure consists of discrete mononuclear, neutral and slightly distorted octahedral molecules. The octahedron around rhodium consists of two trans -chlorine atoms and four nitrogen atoms from the two bidentate amine oxime ligands. The complex formed in situ with the bifunctional ligand I gives up to 95% yield with 105 Rh in pH 9 bicarbonate buffer. This complex was converted to the isothiocyanate derivative with thiophosgene and extracted into CHCl 3 (91%). Conjugation yields of greater than 90% could be obtained with human γ-globulin. The protein conjugation method described is suitable for the preparation of 105 Rh labelled antibodies with specific activities of 1.6–9.3 mCi mg −1 .