Abstract
A new, general synthetic route to 2(1 H)-pyrazinones 11 is described. The four-step synthesis is accomplished utilizing a regioselective hydrolysis and N-alkylation. These compounds efficiently undergo metal-catalyzed cross-coupling reactions to install P2 diversity groups in the 6-position, which can be used to refine the SAR of the S2 pocket of the Tissue Factor/Factor VIIa (TF/VIIa) complex.
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