Synthesis and crystal structures of substituted benzenes and benzoquinones as tissue factor VIIa inhibitors

…, AM Stevens, RA Stegeman, WC Stallings…

Index: Parlow, John J.; Stevens, Anna M.; Stegeman, Roderick A.; Stallings, William C.; Kurumbail, Ravi G.; South, Michael S. Journal of Medicinal Chemistry, 2003 , vol. 46, # 20 p. 4297 - 4312

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Citation Number: 45

Abstract

Several multistep syntheses of substituted benzenes are reported. The benzene analogues were designed such that their substitution pattern would occupy and interact with the S1, S2, and S3 pockets of the tissue Factor VIIa enzyme. A variety of chemical transformations including nucleophilic additions, reductive aminations, Stille couplings, and polymer- assisted solution-phase (PASP) techniques were used to prepare key intermediates and ...