Dianhydrohexitole-Based Benzamidines: An Efficient Synthesis of New Factor

Dianhydrohexitole-based benzamidines were synthe- sised as potential factor Xa inhibitors. The key steps for the synthe- sis of a bis-benzamidine series were nucleophilic aromatic substitutions and Mitsunobu reactions to introduce substituted phe- nyl ether moieties. Mono-benzamidines with an ortho-substituted biphenyl group were prepared using a Negishi-type cross coupling procedure. The benzamidines showed high biological activity and selectivity for factor Xa inhibition.