Synthesis of 2-pyridones as tissue factor VIIa inhibitors
2-Pyridones were prepared from 2,6-dibromopyridine via a multi-step synthesis. A variety of chemical transformations, including regioselective nucleophilic addition and selective nitrogen alkylation, afforded the penultimate intermediate 9. A combination of two-dimensional NMR techniques to unequivo...
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Published in | Tetrahedron Vol. 59; no. 39; pp. 7695 - 7701 |
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Main Authors | , |
Format | Journal Article |
Language | English |
Published |
OXFORD
Elsevier Ltd
22.09.2003
Elsevier |
Subjects | |
Online Access | Get full text |
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Summary: | 2-Pyridones were prepared from 2,6-dibromopyridine via a multi-step synthesis. A variety of chemical transformations, including regioselective nucleophilic addition and selective nitrogen alkylation, afforded the penultimate intermediate 9. A combination of two-dimensional NMR techniques to unequivocally assign the structure of 9 is described. Compound 9 was then used in a Suzuki coupling and further derivatized to afford the targeted tissue Factor VIIa inhibitors. These compounds were tested in several serine protease enzyme assays with biological activity reported.
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ISSN: | 0040-4020 1464-5416 |
DOI: | 10.1016/S0040-4020(03)01239-0 |