- An efficient multikilogram synthesis of ABT-963: A selective COX-2 inhibitor
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An efficient chemical process for the multikilogram synthesis of ABT-963 (3) is described. The potent and selective COX-2 inhibitor was prepared in four steps in 36% overall isolated yield from commercially available 3,4-difluoroaniline (4). The chemistry, which required no chromatography, involved a facile one-pot synthesis of the pyridazinone core, a selective alkoxylation, a high yielding Suzuki coupling, and a very efficient oxidation.
- Kerdesky, Francis A. J.,Leanna, M. Robert,Zhang, Ji,Li, Wenke,Lallaman, John E.,Ji, Jianguo,Morton, Howard E.
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p. 512 - 517
(2012/12/22)
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- Confirmation and prevention of halogen exchange: practical and highly efficient one-pot synthesis of dibromo- and dichloropyridazinones
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Commercially available anilines were converted by a two step, one-pot process to the corresponding pyridazinones in good to excellent yields. During the process research, a significant halogen exchange was confirmed and prevented which allowed the process to be scaled to multikilogram quantities.
- Zhang, Ji,Morton, Howard E.,Ji, Jianguo
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p. 8733 - 8735
(2007/10/03)
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- Prostaglandin endoperoxide H synthase biosynthesis inhibitors
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The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).
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