Potent thrombin inhibitors via a 20-membered ring olefin metathesis macrocyclization

Abstract

Twenty-membered ring pyrazinone derived macrocycles were prepared as a means to enhance the potency of existing thrombin inhibitors. Macrocyclization was accomplished via Grubbs olefin metathesis of a highly functionalized allyl-alloc scaffold, thus further confirming the power of such methodology.