This article describes a simple method for the synthesis of roxifiban, a potent glycoprotein GP IIb-IIIa receptor antagonist, by a diastereoselective coupling approach to give .99.9% optical purity. We have also described an attempt to resolve the key synthetic intermediate by diastereomeric ester formation. Although we have been able to separate two diastereomeric esters, the removal of the chiral auxiliary led to partial racemization.
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