Solid-Phase Synthesis of Amidine-Based GP IIb-IIIa Antagonists on Dendrimer Resin Beads

Many amidine-based molecules are known to be antagonists of the fibrinogen−GP IIb-IIIa interaction, therefore useful in the treatment of thrombotic deseases. Here we report the solid-phase synthesis of a small library of amidines, starting from high-loading dendrimerised TentaGel beads, using resin-bound 4-amidinobenzoic acid as a template. These compounds mimic the structure of known active compounds like Lamifiban (Ro44-9883) and TAK-029; the first solid-phase synthesis of which is also reported in this paper.