Dianhydrohexitole-Based Benzamidines: An Efficient Synthesis of New Factor Xa Inhibitors

Dianhydrohexitole-Based Benzamidines: An Efficient Synthesis of New Factor Xa Inhibitors

ABSTRACT Dianhydrohexitole-based benzamidines were synthesised as potential factor Xa inhibitors. The key steps for the synthesis of a bis-benzamidine series were nucleophilic aromatic substitutions and Mitsunobu reactions to introduce substituted phenyl ether moieties. Mono-benzamidines with an ORT...

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Veröffentlicht in:Synthesis (Stuttgart) 2004-06, Vol.2004 (8), p.1211-1228
Hauptverfasser: Vogler, Marko, Koert, Ulrich, Harms, Klaus, Dorsch, Dieter, Gleitz, Johannes, Raddatz, Peter
Format: Artikel
Sprache:eng
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Zusammenfassung:ABSTRACT Dianhydrohexitole-based benzamidines were synthesised as potential factor Xa inhibitors. The key steps for the synthesis of a bis-benzamidine series were nucleophilic aromatic substitutions and Mitsunobu reactions to introduce substituted phenyl 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.
ISSN:0039-7881
1437-210X
DOI:10.1055/s-2004-822356