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A new solid-phase labeling strategy for the preparation of (99m)Tc and Re chelate complexes and associated peptide derivatives, was developed. Resin-bound monoamide monoamine (MAMA) chelates were prepared in such a manner that upon the addition of a suitable Re(V) and Tc(V) precursor the target metal complexes were selectively released from the resin. The desired products were isolated from unreacted ligand by a simple filtration/solid-phase extraction procedure. In addition to the preparation of a series of functionalized ligands, a peptide conjugate was constructed from one of the resin-bound chelates using a conventional automated peptide synthesizer. The yields of the Re chelate complexes were typically greater than 70%, while the maximum yield for reactions run at the tracer level using (99m)Tc was 50%. The reported approach has a number of attractive features, including the opportunity to prepare libraries of novel agents, the ability to isolate macroscopic amounts of Re complexes for use in in vitro screening studies and as well-characterized standards for tracer level work, and the ability to produce (99m)Tc complexes that are free of any unreacted starting material without having to employ preparative HPLC.

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The Biosynthesis of Pramanicin: Origin of the Carbon Skeleton. -Incorporation of labeled acetates and serine into pramanicin (I) shows that its carbon skeleton is derived from eight acetate units and a serine residue, implying that the biosynthesis proceeds via an acyl-tetramic acid intermediate. -(HARRISON, P. H. M.; HUGHES, D. W.; RIDDOCH, R. W.; Chem. Commun. (Cambridge) (1998) 2, 273-274; Dep. Chem., McMaster Univ., Hamilton, Ont. L8S 4M1, Can.; EN)